First hyperpolarizability in a new benzimidazole derivative

International Nuclear Information System (INIS)

Rodembusch, Fabiano Severo; Buckup, Tiago; Segala, Maximiliano; Tavares, Luciana; Correia, Ricardo Rego Bordalo; Stefani, Valter

2004-01-01

A new benzimidazole, 2-(4'-amino-2'-hydroxyphenyl)-6-nitrobenzimidazole (LEN), with promising applications in nonlinear optics were synthesized, purified and characterized by classical techniques. The UV-Vis and steady-state fluorescence of LEN in solution were applied in order to characterize the photophysical behaviour of this new fluorescent dye. The Hyper-Rayleigh Scattering study indicates a remarkable increase in the β absolute value (1197.3 ± 1.2 x 10 -30 esu) of the LEN in acetone at 1064 nm, when comparing with a previously described benzoxazole (BO6). The ratio between the experimental β and the maximum theoretical value using a two-level model was also improved by a factor 6. Ab initio and semi-empirical calculations of the dipole moments and the first hyperpolarizability are also presented. The enhancement in the experimental hyperpolarizability value in relation to BO6 is explained in terms of the benzimidazolic ring basicity and a prototropic effect (annular tautomerism) present in the LEN, identified as a resonance-assisted hydrogen bond, which leads to a stronger electronic delocalization

Dibromido[1,1′-dibutyl-2,2′-(pentane-1,1-diyldi-1H-benzimidazole]copper(II

Directory of Open Access Journals (Sweden)

Robert T. Stibrany

2010-07-01

Full Text Available In the title compound, [CuBr2(C27H36N4], the CuII ion exhibits a distorted tetrahedral coordination geometry provided by two bromide ions and by chelation of two imine N-atom donors from a bis(benzimidazole ligand. Chelation results in a six-membered boat-shaped ring which links the benzimidazole groups. Each bis(benzimidazole fragment contains three n-butyl substituents, two of which have the expected trans conformation; the third exhibits the higher-energy cis conformation, an orientation consistent with several short intramolecular C—H...Br interactions. Essentially planar (r.m.s. deviations of 0.0101 and 0.0183 Å benzimidazole groups are oriented so as to give the bis(benzimidazole fragment a V-shaped appearance in profile with the cis and trans n-butyl groups directed to opposite sides of the planes. In the crystal, columns of molecules along the b-axis direction form layers parallel to the (202 planes. Within a given column, the molecules are linked by C—H...Br hydrogen bonds. The molecules in adjacent columns are also linked by intermolecular C—H...π interactions, forming a three-dimensional network.

Synthesis of Aminofuran-Linked Benzimidazoles and Cyanopyrrole-Fused Benzimidazoles by Condition-Based Skeletal Divergence.

Science.gov (United States)

Hsu, Wei-Shun; Tsai, Min-Huan; Barve, Indrajeet J; Yellol, Gorakh S; Sun, Chung-Ming

2017-07-10

A condition-based skeletal divergent synthesis was explored to achieve skeletal diversity in two component condensation reaction. Cyanomethyl benzimidazole was reacted with α-bromoketone under thermal conditions to furnish 2-aminofuranyl-benzimidazoles, while the same reaction afforded 3-cyano-benzopyrrolo-imidazoles under microwave irradiation. Two nonequivalent nucleophilic centers on benzimidazole moiety were manipulated elegantly by different reaction conditions to achieve the skeletal diversity.

Structural Modifications of Benzimidazoles via Multi-Step Synthesis and Their Impact on Sirtuin-Inhibitory Activity.

Science.gov (United States)

Yoon, Yeong Keng; Choon, Tan Soo

2016-01-01

Benzimidazole derivatives have been shown to possess sirtuin-inhibitory activity. In the continuous search for potent sirtuin inhibitors, systematic changes on the terminal benzene ring were performed on previously identified benzimidazole-based sirtuin inhibitors, to further investigate their structure-activity relationships. It was demonstrated that the sirtuin activities of these novel compounds followed the trend where meta-substituted compounds possessed markedly weaker potency than ortho- and para-substituted compounds, with the exception of halogenated substituents. Molecular docking studies were carried out to rationalize these observations. Apart from this, the methods used to synthesize the interesting compounds are also discussed. © 2015 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

Synthesis and optical properties of novel pyrido[1,2-a]benzimidazole-containing 1,3,4-oxadiazole derivatives

International Nuclear Information System (INIS)

Yang He; Ge Yanqing; Jia Jiong; Wang Jianwu

2011-01-01

A series of novel substituted 1,3,4-oxadiazole derivatives containing pyrido[1,2-a]benzimidazole moiety were synthesized and characterized using FTIR, 1 H NMR, 13 C NMR, and HRMS. An efficient tandem reaction was employed as a key step in constructing the pyrido[1,2-a]benzimidazole moiety under very mild condition. The structure of compound 4a was established by X-ray crystallography. The UV-vis absorption and fluorescence spectral characteristics of these compounds were investigated in several solvents. Compounds 4a-i display similar absorptions, with absorption peaks ranging from 330 to 339 nm in acetonitrile, while the absorption maxima of compound 4j bearing a diphenylamino group on the benzene ring is red-shifted distinctly to 377 nm due to the strong electron-donating property of its substituent and extended π-conjugated system. All these target heterocyclic compounds present blue-green emissions (461-487 nm) in dilute solutions and show high quantum yields of fluorescence (φ PL =0.65-0.99) in dichloromethane. - Research Highlights: → The first report about the unique optical properties of pyrido[1,2-a]benzimidazole heteroaromatic compounds containing 1,3,4-oxadiazole unit. → Synthesis of pyrido[1,2-a]benzimidazole moiety via a novel efficient tandem reaction. → The target heterocyclic compounds showing high quantum yields of fluorescence, with great potential for use as fluorescent pigments and in optical/electro devices.

Synthesis of ruthenium (III) complexes with benzimidazole derivatives

International Nuclear Information System (INIS)

Vyas, P.C.; Chahar, Yogesh K.; Garg, Yajula; Seth, Gita

2003-01-01

Complexes of ruthenium with biologically important benzimidazole derivatives, viz. 2-(2'-hydroxyphenyl) benzimidazole (HOPBI), 2-2'- mercaptophenyl) benzimidazole (HSPBI), 2- (2'-hydroxynaphthyl) benzimidazole (HONBI) have been synthesized and characterized. (author)

Novel benzimidazole derivatives as corrosion inhibitors of mild steel in the acidic media. Part II: Theoretical studies

International Nuclear Information System (INIS)

Cao, Ziyi; Tang, Yongming; Cang, Hui; Xu, Jinqiu; Lu, Gang; Jing, Wenheng

2014-01-01

Highlights: • Quantum chemical and MD studies of benzimidazole derivatives inhibitors. • Inhibition effectiveness depends on the ability to accept electrons. • Active sites of adsorption are mainly centralized on imidazole rings. • Steric effect results in the non-planar adsorption of BBIA and TBIA. - Abstract: In this paper, the adsorption behavior and inhibition mechanism of 2-aminomethyl benzimidazole (ABI), bis(2-benzimidazolylmethyl) amine (BBIA) and tri-(2-benzimidazolylmethyl) amine (TBIA) on the surface of mild steel were studied by quantum chemical calculations and molecular dynamics (MD) simulations. It was found that the three molecules show the similar ability to donate electrons while the difference in inhibition performance should mainly be attributed to the difference in accepting electrons. MD simulations show that steric effect between the benzimidazole segments significantly affects the adsorptive configurations of the molecules on Fe (1 0 0) surface

ANTIBACTERIAL ACTIVITY OF BENZIMIDAZOLES 2-THIO, 2-AMINODERIVATIVES AND COMPLEXES OF BENZIMIDAZOLES WITH TRANSITIONAL METALS

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E. I. Mayboroda

2014-01-01

Full Text Available The literature data about antibacterial properties of benzimidazole 2-thio-, 2-aminoderivatives and benzimidazole complexes have been generalized and systematized in the review. Today prevention and treatment of diseases caused by microorganisms is an actual problem of modern therapy. Therefore, the search for active molecules, the based on them development of some new, more effective antimicrobial agents is an important task of modern pharmaceutical chemistry. Promising compounds for solving these problems are benzimidazole derivatives. They are available, functionally capable, stable and have a wide spectrum of biological activities (antiviral, anthelmintic, antibacterial, anticancer, antidiabetic.The purpose of this paper is to generalize and systematize information about the antimicrobial action of 2-thio-, 2-amino-substituted benzimidazoles and benzimidazole derivatives complexes with transition metals.These compounds and their complexes with transition metals are active against pathogenic strains Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus, Salmonella typhimurium, Proteus vulgaris, Bacillus cereus, Micrococcus luteus, Helicobacter рylori and others.

Novel trisubstituted benzimidazoles, targeting Mtb FtsZ, as a new class of antitubercular agents.

Science.gov (United States)

Kumar, Kunal; Awasthi, Divya; Lee, Seung-Yub; Zanardi, Ilaria; Ruzsicska, Bela; Knudson, Susan; Tonge, Peter J; Slayden, Richard A; Ojima, Iwao

2011-01-13

Libraries of novel trisubstituted benzimidazoles were created through rational drug design. A good number of these benzimidazoles exhibited promising MIC values in the range of 0.5-6 μg/mL (2-15 μM) for their antibacterial activity against Mtb H37Rv strain. Moreover, five of the lead compounds also exhibited excellent activity against clinical Mtb strains with different drug-resistance profiles. All lead compounds did not show appreciable cytotoxicity (IC(50) > 200 μM) against Vero cells, which inhibited Mtb FtsZ assembly in a dose dependent manner. The two lead compounds unexpectedly showed enhancement of the GTPase activity of Mtb FtsZ. The result strongly suggests that the increased GTPase activity destabilizes FtsZ assembly, leading to efficient inhibition of FtsZ polymerization and filament formation. The TEM and SEM analyses of Mtb FtsZ and Mtb cells, respectively, treated with a lead compound strongly suggest that lead benzimidazoles have a novel mechanism of action on the inhibition of Mtb FtsZ assembly and Z-ring formation.

Benzimidazole and imidazole hexachlorocerates

Energy Technology Data Exchange (ETDEWEB)

Bayanov, A P; Burylev, B P; Temerdashev, Z A; Gusev, V I [Kubanskij Gosudarstvennyj Univ., Krasnodar (USSR)

1983-02-01

The process of hexachlorocerium acid with benzimidazole and imidazole interaction and the reaction products are investigated. The values of thermodynamic characteristics of the hexachlorocerium acid reaction with benzimidazole are equal: ..delta..Gsub(298K)=-16.5+-0.2 kJ/mol, ..delta..Hsub(298K)=-63.6+-0.8 kJ/mol, ..delta..Ssub(298K)=-157+-5 J/mol degrees. By the IR spectroscopy and radiography method the individuality of separated compounds has been found. The thermal stability of compounds is determined. The temperature dependence of splitting off chlorine atom from benzimidazole hexachlorocerate on pressure is investigated. Thermodynamic characteristics and activation energies of the process are calculated.

Benzimidazole and imidazole hexachlorocerates

International Nuclear Information System (INIS)

Bayanov, A.P.; Burylev, B.P.; Temerdashev, Z.A.; Gusev, V.I.

1983-01-01

The process of hexachlorocerium acid with benzimidazole and imidazole interaction and the reaction products are investigated. The values of thermodynamic characteristics of the hexachlorocerium acid reaction with benzimidazole are equal: ΔGsub(298K)=-16.5+-0.2 kJ/mol, ΔHsub(298K)=-63.6+-0.8 kJ/mol, ΔSsub(298K)=-157+-5 J/mol degrees. By the IR spectroscopy and radiography method the individuality of separated compounds has been found. The thermal stability of compounds is determined. The temperature de-- pendence of splitting off chlorine atom from benzimidazole hexachlorocerate on pressure is investigated. Thermodynamic characteristics and activation energies of the process are calculated

Synthesis, antimicrobial and cytotoxic activity of novel azetidine-2-one derivatives of 1H-benzimidazole

Directory of Open Access Journals (Sweden)

Malleshappa Noolvi

2014-04-01

Full Text Available A series of 1-methyl-N-[(substituted-phenylmethylidene-1H-benzimidazol-2-amines (4a–4g were prepared via the formation of 1-methyl-1H-benzimidazol-2-amine (3, which was prepared by the cycloaddition of o-phenylenediamine (1 with cyanogen bromide in the presence of aqueous base followed by N-methylation with methyl iodide in the presence of anhydrous potassium carbonate in dry acetonitrile. Moreover, the four-membered β-lactam ring was introduced by the cycloaddition of 4a–4g and chloroacetyl chloride in the presence of triethylamine catalyst to give 3-chloro-1-(1-methyl-1H-benzimidazol-2-yl-(4′-substituted-phenylazetidin-2-one 5a–5g. A total of 14 compounds were synthesized and characterized by IR, 1H NMR, 13C NMR and Mass spectral technique, in addition they were evaluated for anti-bacterial and cytotoxic properties. Among the chemicals tested 4a, 4b, 5a, 5b, 5g exhibited good antibacterial activity and 5f, 5g shown good cytotoxic activity in vitro.

The therapeutic journey of benzimidazoles: a review.

Science.gov (United States)

Bansal, Yogita; Silakari, Om

2012-11-01

Presence of benzimidazole nucleus in numerous categories of therapeutic agents such as antimicrobials, antivirals, antiparasites, anticancer, anti-inflammatory, antioxidants, proton pump inhibitors, antihypertensives, anticoagulants, immunomodulators, hormone modulators, CNS stimulants as well as depressants, lipid level modulators, antidiabetics, etc. has made it an indispensable anchor for development of new therapeutic agents. Varied substitutents around the benzimidazole nucleus have provided a wide spectrum of biological activities. Importance of this nucleus in some activities like, Angiotensin I (AT(1)) receptor antagonism and proton-pump inhibition is reviewed separately in literature. Even some very short reviews on biological importance of this nucleus are also known in literature. However, owing to fast development of new drugs possessing benzimidazole nucleus many research reports are generated in short span of time. So, there is a need to couple the latest information with the earlier information to understand the current status of benzimidazole nucleus in medicinal chemistry research. In the present review, various derivatives of benzimidazole with different pharmacological activities are described on the basis of substitution pattern around the nucleus with an aim to help medicinal chemists for developing an SAR on benzimidazole derived compounds for each activity. This discussion will further help in the development of novel benzimidazole compounds. Copyright © 2012 Elsevier Ltd. All rights reserved.

Synthesis and photophysical characterizations of thermal-stable naphthalene benzimidazoles.

Science.gov (United States)

Erten-Ela, Sule; Ozcelik, Serdar; Eren, Esin

2011-07-01

Microwave-assisted synthesis, photophysical and electrochemical properties of thermal-stable naphthalene benzimidazoles and naphthalimides are studied in this paper. Microwave-assisted synthesis of naphthalene benzimidazoles provide higher yields than the conventional thermal synthesis. Comparative photophysical properties of naphthalene benzimidazoles and naphthalimides are revealed that conjugation of electron-donating group onto naphthalimide moiety increases fluorescence quantum yields. Fluorophore-solvent interactions are also investigated using Lippert-Mataga equation for naphthalimides and naphthalene benzimidazoles. Thermal stabilities of naphthalene benzimidazoles are better than naphthalimides due to increased aromaticity. The experimental E(LUMO) levels of naphthalene benzimidazoles are found to be between 3.15 and 3.28 eV. Therefore, naphthalene benzimidazole derivatives consisting of anchoring groups are promising materials in organic dye sensitized solar cells. © Springer Science+Business Media, LLC 2011

Synthesis and characterisation of ruthenium(III) complexes with benzimidazole derivatives

International Nuclear Information System (INIS)

Vyas, P.C.; Kaur, N.; Goel, A.K.; Vyas, S.

1995-01-01

Complexes of ruthenium trichloride with biologically important benzimidazole derivatives, viz., 2-(hydroxy methyl) benzimidazole, 2-(l-hydroxy ethyl) benzimidazole, 2-(mercapto methyl) benzimidazole, 2-(l-mercapto ethyl) benzimidazole, and 2,2'-bis-benzimidazole have been synthesized by reacting the above metal chloride and ligands respectively in 1:3 molar ratio. These complexes are characterised on the basis of elemental analysis, molar conductance data, room temperature, magnetic moment values, electronic spectral and IR spectral studies. (author). 17 refs., 2 tabs

Design, synthesis and biological evaluation of novel hydroxy-phenyl-1H-benzimidazoles as radical scavengers and UV-protective agents.

Science.gov (United States)

Bino, Alessia; Baldisserotto, Anna; Scalambra, Emanuela; Dissette, Valeria; Vedaldi, Daniela Ester; Salvador, Alessia; Durini, Elisa; Manfredini, Stefano; Vertuani, Silvia

2017-12-01

An ever-increasing incidence of skin neoplastic diseases is registered. Therefore, it is important to protect the skin from the UV radiation that reaches the epidermis and dermis but also to block ROS generated by them. Our attention was attracted in developing new compounds provided with both UV filtering and antioxidant capacities. To this end, 2-phenyl-1H-benzimidazole-5-sulfonic acid (PBSA), a known UV filter, was selected as lead compound for its lack of antioxidant activity, high water solubility and good safety profile. PBSA was sequentially modified introducing hydroxyls on the phenyl ring and also substituting the functional group in position 5 of the benzimidazole ring. At the end of the synthetic study, a new, very potent class of antioxidants has been obtained. Surprisingly some of the developed molecules, while devoid of significant UV-filtering activity was endowed with potent UV-filtering booster capability if associated with known commercial UVB and UVA filters.

Synthesis of 2-arylidenebenzocycloalkanones containing N-donor heterocyclic rings

Energy Technology Data Exchange (ETDEWEB)

Sun, S.-W., E-mail: sunsw0819@163.com [Yuncheng University, Department of Applied Chemistry (China); Zhang, X., E-mail: zhangx@hit.edu.cn [Harbin Institute of Technology, Academy of Fundamental and Interdisciplinary Science (China); Wang, G.-F. [Yuncheng University, Department of Applied Chemistry (China)

2016-12-15

A series of 2-arylidenebenzocycloalkanones containing heterocyclic rings 1–8 were prepared and characterized by IR, {sup 1}H NMR and elemental analyses. X-ray diffraction study of 6 reveals that the cyclohexyl ring of the 3,4-dihydronaphthalen-1(2H)-one adopts a chair conformation with a maximum deviation of 0.547(3) Å and makes dihedral angles of 52.24(17)° and 11.23(16)°, respectively, with the benzene plane and the mean plane of the benzimidazole ring.

Novel organic dyes based on phenyl-substituted benzimidazole for dye sensitized solar cells

Energy Technology Data Exchange (ETDEWEB)

Saltan, Gözde Murat [Department of Chemistry, Faculty of Arts and Science, Celal Bayar University, Yunus Emre, 45140 Manisa (Turkey); Dinçalp, Haluk, E-mail: haluk.dincalp@cbu.edu.tr [Department of Chemistry, Faculty of Arts and Science, Celal Bayar University, Yunus Emre, 45140 Manisa (Turkey); Kıran, Merve; Zafer, Ceylan [Solar Energy Institute, Ege University, Bornova, 35100 Izmir (Turkey); Erbaş, Seçil Çelik [Celal Bayar University, Materials Engineering Department, Faculty of Engineering, Yunus Emre, 45140 Manisa (Turkey)

2015-08-01

Two new sensitizers derived from benzimidazole core for dye-sensitized solar cell (DSSC) applications were designed and synthesized as D–π–A structures, in which two phenyl-substituted benzimidazole group, a phenyl ring and a cyanoacrylic acid were used as the electron donor, π-conjugated linkage and the electron acceptor, respectively. Effect of methoxy- and N,N-dimetylamino- moieties attached to the phenyl groups of benzimidazole were investigated by means of optical and photovoltaic measurements. The compounds exhibit broad absorption maximum at 387 nm with the tail extending up to 500 nm on TiO{sub 2}-coated thin film. The longer wavelength absorption band around 360 nm and the much longer decay components could be attributed to the existence of charge transfer state of the dyes in solutions. DSSC device fabricated by using methoxy substituted dye (BI5a) as a sensitizer shows much better incident photon-to-current conversion efficiency (IPCE) of 64% giving cell efficiency of 2.68%. - Graphical abstract: Display Omitted - Highlights: • Long decay times suggest the delayed fluorescence caused by the existence of ICT. • The best solar energy conversion efficiency was obtained for BI5a dye (2.68%). • More fluorescent BI5a dye gives higher photocurrent generation.

Novel organic dyes based on phenyl-substituted benzimidazole for dye sensitized solar cells

International Nuclear Information System (INIS)

Saltan, Gözde Murat; Dinçalp, Haluk; Kıran, Merve; Zafer, Ceylan; Erbaş, Seçil Çelik

2015-01-01

Two new sensitizers derived from benzimidazole core for dye-sensitized solar cell (DSSC) applications were designed and synthesized as D–π–A structures, in which two phenyl-substituted benzimidazole group, a phenyl ring and a cyanoacrylic acid were used as the electron donor, π-conjugated linkage and the electron acceptor, respectively. Effect of methoxy- and N,N-dimetylamino- moieties attached to the phenyl groups of benzimidazole were investigated by means of optical and photovoltaic measurements. The compounds exhibit broad absorption maximum at 387 nm with the tail extending up to 500 nm on TiO 2 -coated thin film. The longer wavelength absorption band around 360 nm and the much longer decay components could be attributed to the existence of charge transfer state of the dyes in solutions. DSSC device fabricated by using methoxy substituted dye (BI5a) as a sensitizer shows much better incident photon-to-current conversion efficiency (IPCE) of 64% giving cell efficiency of 2.68%. - Graphical abstract: Display Omitted - Highlights: • Long decay times suggest the delayed fluorescence caused by the existence of ICT. • The best solar energy conversion efficiency was obtained for BI5a dye (2.68%). • More fluorescent BI5a dye gives higher photocurrent generation

Recyclization reactions leading to benzimidazoles

Science.gov (United States)

Mamedov, Vakhid A.; Murtazina, Anna M.

2011-05-01

The published data on the recyclization reactions that afford benzimidazoles are generalized and systematized. Both classical and new methods of benzimidazole synthesis are considered. Attention is focused on the publications over the recent 10-15 years; of the earlier publications, only those unknown to the wide circle of chemists are analyzed.

Recyclization reactions leading to benzimidazoles

International Nuclear Information System (INIS)

Mamedov, Vakhid A; Murtazina, Anna M

2011-01-01

The published data on the recyclization reactions that afford benzimidazoles are generalized and systematized. Both classical and new methods of benzimidazole synthesis are considered. Attention is focused on the publications over the recent 10-15 years; of the earlier publications, only those unknown to the wide circle of chemists are analyzed.

Simple, mild, and highly efficient synthesis of 2-substituted benzimidazoles and bis-benzimidazoles

OpenAIRE

Eren,Bilge; Bekdemir,Yunus

2014-01-01

A new convenient method for preparation of 2-substituted benzimidazoles and bis-benzimidazoles is presented. In this method, o-phenylenediamines were condensed with bisulfite adducts of various aldehydes and di-aldehydes under neat conditions by microwave heating. The results were also compared with results of synthesis by conventional heating under reflux. Structures of the products were confirmed by infrared, ¹H- and 13C-NMR spectroscopy. Short reaction times, good yields, easy purification...

Poly(imide benzimidazole)s for high temperature polymer electrolyte membrane fuel cells

DEFF Research Database (Denmark)

Yuan, Sen; Guo, Xiaoxia; Aili, David

2014-01-01

A series of poly(imide benzimidazole) random copolymers (PIBIs) was synthesized by condensation polymerization of biphenyl-4,4'-diyldi(oxo)-4,4'-bis(1,8-naphthalenedicarboxylic anhydride) (BPNDA), 2-(4-aminophenyl)-5-aminobenzimidazole (APABI) and 4,4'diaminodiphenyl ether (ODA) in m-cresol in th......A series of poly(imide benzimidazole) random copolymers (PIBIs) was synthesized by condensation polymerization of biphenyl-4,4'-diyldi(oxo)-4,4'-bis(1,8-naphthalenedicarboxylic anhydride) (BPNDA), 2-(4-aminophenyl)-5-aminobenzimidazole (APABI) and 4,4'diaminodiphenyl ether (ODA) in m...

Synthesis of Some Benzimidazole-substituted Benzotriazoles

African Journals Online (AJOL)

NJD

2-Alkylsubstituted benzimidazoles (3a–h) were prepared from the acid-catalyzed reaction of 4-methyl-1,2-phenylenediamine with corresponding carboxylic acids. Addition of these benzimidazoles to N-chloromethylbenzotriazole in the presence of sodium amide under reflux conditions gave the novel ...

Synthesis, biological evaluation and molecular modeling investigation of some new Benzimidazole analogs as antiviral agents

International Nuclear Information System (INIS)

Goda, Fatma E.; Tantawy, Atif S.; Abou-Zeid, Laila A.; Badr, Sahar M.; Selim, Khalid B.

2008-01-01

A set heterocyclic benzimidazole derivatives bearing 1, 3, 5-triazine group with different substituents at C-2 and C-5 of the benzimidazole ring have been synthesized and evaluated for their antiviral activities against HASV-1. The structures of these compounds have been established by analytical data, IR spectra, H NMR and mass spectra. Compounds 8a and 8b proved to be the most active antiherpetic agents in this study, at EC 50% concentrations of 2.9. 3.4 mg/ml, respectively. Computational evaluation of the quantum chemical descriptors such as hydrphobicity (log P), HOMO-LUMO and the gap energy were calculated and correlated with the antiviral activity. The tested compounds showed proper degree of hydrophobicity ( 5). The HOMO-LUMO gap energy values of the tested compounds are comparable with the observed values for the antiviral drug Acyclovir. (author)

[Benzimidazole and its derivatives--from fungicides to designer drugs. A new occupational and environmental hazards].

Science.gov (United States)

Lutz, Piotr

2012-01-01

Benzimidazole and benzimidazole derivatives play an important role in controlling various fungal pathogens. The benzimidazoles are also used to treat nematode and trematode infections in humans and animals. It acts by binding to the microtubules and stopping hyphal growth. It also binds to the spindle microtubules and blocks nuclear division. The most popular fungicide is carbendazim. The fungicide is used to control plant diseases in cereals and fruits. Laboratory studies have shown that carbendazim cause infertility and destroy the testicles of laboratory animals. Other benzimidazole derivatives are used as a preservative in paint, textile, papermaking, leather industry, and warehousing practices, as well as a preservative of fruits. Occupational exposure to benzimidazole may occur through inhalation and dermal contact with those compounds at workplaces where benzimidazole is used or produced. Some of the benzimidazoles are common environmental pollutants. They are often found in food and fruit products. Some of the benzimidazoles, like a astemizole or esomeprazole have found applications in diverse therapeutical areas. Despite of the clear advantages afforded by the use of benzimidazole derivatives, they share a danger potential. The most hazardous, however, are new illegally synthesed psychoactive drugs known as designer drugs. Some of them, like nitazene, etonitazene or clonitazene belong to benzimidazole derivatives. Laboratory animal studies revealed that etonitazene produced very similar effects in central nervous system as those observed after morphine administration. Considering etonitazene's properties, it seems reasonable to expected that long-term exposure to other benzimidazole derivatives may result in drug abuse and development of drug dependence.

Voltammetric Determination of a Benzimidazole Anthelmintic Mixture ...

African Journals Online (AJOL)

2002-10-17

Oct 17, 2002 ... Electrochemistry, square-wave voltammetry, benzimidazole anthelmintics, ... potential application, cathodic reduction/anodic oxidation, the type of the electrode ... benzimidazole anthelmintic in 10 cm3 of methanol-formic acid.

Structure of substituted 2-(phenoxy)benzimidazoles

Science.gov (United States)

Pavlova, I. S.; Pervova, I. G.; Lipunova, G. N.; Novikova, R. K.; Slepukhin, P. A.; Lipunov, I. N.

2013-03-01

The synthesis and X-ray diffraction study of 1-benzyl-2-[2-(5-ethyltetrazole-2-yl)-phenoxy]-1H-benzimidazole and 1-benzyl-2-[2-(5-ethyltetrazole-2-yl)-4-nitrophenoxy]-1H-benzimidazole single crystals have been performed. The oxidative splitting of an azo-hydrazone group of 1-(2-hydroxy-(5-nitro)phenyl)-3-ethyl-5-(benzylbenzimidazolyl)formazans, a break in the C2-N1 bond, the interaction of o-hydroxyl group of aryl fragment with oxygen, and the formation of new 2-(phenoxy)benzimidazoles are found to occur in the presence of perchlorate iron(III).

Spektrální vlastnosti benzimidazolů

OpenAIRE

Lukešová, Marie

2010-01-01

Spectral Properties of Benzimidazoles Marie Lukešová Charles University in Prague, Faculty of Pharmacy in Hradec Králové Department of Biophysics and Physical Chemistry Abstract: This diploma thesis deals with the spectral properties of benzimidazoles. Most of benzimidazoles are anthelmintic active drug, used primarily in veterinary medicine. Some substances are used as fungicides. The main aim of this study was to clarify the influence of solvents on the absorption spectra and especially on ...

Data on the effects of imidazo[1,2-a]benzimidazole and pyrimido[1,2-a]benzimidazole compounds on intraocular pressure of ocular normotensive rats

Directory of Open Access Journals (Sweden)

Adrian Julian Marcus

2018-06-01

Full Text Available This data is to document the intraocular pressure (IOP lowering activity of imidazo[1,2-a]benzimidazole and pyrimido[1,2-a]benzimidazole compounds in ocular normotensive rats. Effects of single drop application of imidazo[1,2-a]benzimidazole and pyrimido[1,2-a]benzimidazole compounds on IOP in ocular normotensive rats are presented at 3 different concentrations (0.1%, 0.2% and 0.4%. Time course of changes in IOP is presented over 6 h period post-instillation. The IOP lowering activities of test compounds were determined by assessing maximum decrease in IOP from baseline and corresponding control, duration of IOP lowering and area under curve (AUC of time versus response curve. Data shown here may serve as benchmarks for other researchers studying IOP-lowering effect of imidazo[1,2-a]benzimidazole and pyrimido[1,2-a]benzimidazole compounds and would be useful in determining therapeutic potential of these test compounds as IOP lowering agents. Keywords: Drug screening, Intraocular pressure, Intraocular pressure lowering activity, Imidazo[1,2-a]benzimidazoles, Pyrimido[1,2-a]benzimidazoles, Ocular normotensive rats, Rebound tonometry

Simple, mild, and highly efficient synthesis of 2-substituted benzimidazoles and bis-benzimidazoles

International Nuclear Information System (INIS)

Eren, Bilge; Bekdemir, Yunus

2014-01-01

A new convenient method for preparation of 2-substituted benzimidazoles and bis-benzimidazoles is presented. In this method, o-phenylenediamines were condensed with bisulfite adducts of various aldehydes and di-aldehydes under neat conditions by microwave heating. The results were also compared with results of synthesis by conventional heating under reflux. Structures of the products were confirmed by infrared, 1 H- and 13 C-NMR spectroscopy. Short reaction times, good yields, easy purification of products, and mild reaction conditions are the main advantages of this method. (author)

Simple, mild, and highly efficient synthesis of 2-substituted benzimidazoles and bis-benzimidazoles

Energy Technology Data Exchange (ETDEWEB)

Eren, Bilge, E-mail: bilge.eren@bilecik.edu.tr [Faculty of Science and Arts, Department of Chemistry, Bilecik Seyh Edebali University, (Turkey); Bekdemir, Yunus [Faculty of Science and Arts, Canik Basari University, Samsun (Turkey)

2014-07-01

A new convenient method for preparation of 2-substituted benzimidazoles and bis-benzimidazoles is presented. In this method, o-phenylenediamines were condensed with bisulfite adducts of various aldehydes and di-aldehydes under neat conditions by microwave heating. The results were also compared with results of synthesis by conventional heating under reflux. Structures of the products were confirmed by infrared, {sup 1}H- and {sup 13}C-NMR spectroscopy. Short reaction times, good yields, easy purification of products, and mild reaction conditions are the main advantages of this method. (author)

Simple, mild, and highly efficient synthesis of 2-substituted benzimidazoles and bis-benzimidazoles

Directory of Open Access Journals (Sweden)

Bilge Eren

2014-01-01

Full Text Available A new convenient method for preparation of 2-substituted benzimidazoles and bis-benzimidazoles is presented. In this method, o-phenylenediamines were condensed with bisulfite adducts of various aldehydes and di-aldehydes under neat conditions by microwave heating. The results were also compared with results of synthesis by conventional heating under reflux. Structures of the products were confirmed by infrared, ¹H- and 13C-NMR spectroscopy. Short reaction times, good yields, easy purification of products, and mild reaction conditions are the main advantages of this method.

Study of the {sup 14}C benzimidazole distribution in mice after inter-peritoneal injection; Etude de la repartition du benzimidazole {sup 14}C chez la souris apres injection intraperitoneale

Energy Technology Data Exchange (ETDEWEB)

Tyortyalian, C [Commissariat a l' Energie Atomique, Grenoble (France). Centre d' Etudes Nucleaires

1965-07-01

In order to provide further information on the mechanism of benzimidazole radioprotective activity, this work studies the tissual repartition in mice of this compound labelled with carbon 14. Experiments have showed that benzimidazole distribution is fast and homogeneous in all the tissues, but however affinity appears at the level of stomach and gastric content. Elimination is made through the urinary system and is very fast. (author) [French] Dans le cadre de l'etude du mecanisme de l'action radioprotectrice du benzimidazole, ce travail a pour objet l'etude de la repartition tissulaire chez la souris de ce compose marque au carbone 14. L'experimentation a montre que le benzimidazole se repartit tres rapidement et de facon pratiquement homogene dans tous les tissus, avec toutefois une affinite paraissant se manifester au niveau de l'estomac et du contenu gastrique. L'elimination, qui se fait par voie urinaire, est tres rapide. (auteur)

Novel structural hybrids of pyrazolobenzothiazines with benzimidazoles as cholinesterase inhibitors.

Science.gov (United States)

Aslam, Sana; Zaib, Sumera; Ahmad, Matloob; Gardiner, John M; Ahmad, Aqeel; Hameed, Abdul; Furtmann, Norbert; Gütschow, Michael; Bajorath, Jürgen; Iqbal, Jamshed

2014-05-06

Two series of novel pyrazolobenzothiazine-based hybrid compounds were efficiently synthesized starting from saccharin sodium salt. Pyrazolo[4,3-c][1,2]benzothiazine scaffolds were N-arylated by using p-fluorobenzaldehyde, followed by the incorporation of a benzimidazole or similar ring systems by treatment with arylenediamines. These phenylene-connected hybrid compounds were investigated as potential inhibitors of acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE). Compounds 12d and 12k were the most potent AChE inhibitors with IC50 values of 11 and 13 nM, respectively, while 6j (IC50 = 17 nM) proved to be the most active inhibitor against BuChE with remarkable selectivity for BuChE over AChE. Molecular docking studies were also performed on human AChE and BuChE to suggest possible binding modes in which the inhibitor's extended structure is accommodated along the active site gorge of both enzymes. Copyright © 2014 Elsevier Masson SAS. All rights reserved.

Synthesis and Photophysical Characterizations of Thermal -Stable Naphthalene Benzimidazoles

OpenAIRE

Erten Ela, Şule; Özçelik, Serdar; Eren, Ersin

2011-01-01

Microwave-assisted synthesis, photophysical and electrochemical properties of thermal-stable naphthalene benzimidazoles and naphthalimides are studied in this paper. Microwave-assisted synthesis of naphthalene benzimidazoles provide higher yields than the conventional thermal synthesis. Comparative photophysical properties of naphthalene benzimidazoles and naphthalimides are revealed that conjugation of electron-donating group onto naphthalimide moiety increases fluorescence ...

1-ethyl gallate-2-substituted phenoxymethyl benzimidazoles: synthesis, molecular structure, antimicrobial activities and complex with cr(iii)

International Nuclear Information System (INIS)

Zhao, L.; Wu, J.; Wu, J.; Wang, Z.; Gu, H.

2017-01-01

The design of gallate and benzimidazole containing derivatives is expected to produce new bioactive molecules with multiple applications. Here the synthesis of eight novel benzimidazole compounds containing ethyl gallate and substituted phenoxymethyl units are reported. Firstly, the ring closure reaction between o-phenylendiamine and substituted phenoxyacetic acids resulted in 2-substituted phenoxymethyl benzimidazoles that were then modified by the N-hydroxyethylation with 2-chloroethyl alcohol under a phase transfer catalysis condition. The obtained 1-hydroxyethyl-2-substituted phenoxymethyl benzimidazoles were finally translated into the target title compounds 8a-h by an indirect esterification method in which three O-H groups of gallic acid were first protected by acetyls and deprotected after the esterification reaction by adding hydrazine hydrate. The structures of the title products 8a-h were fully characterized and confirmed by elemental analysis, MS, IR, 1H-NMR, 13C-NMR and single crystal X-ray diffraction techniques. Antimicrobial tests by inhibition zones indicated that these compounds exhibited diverse inhibitory effects against the test bacteria and fungi, and the type and position of the substituent groups in the phenoxymethyl moieties had obvious influence on their antimicrobial activities. Furthermore, the Cr(III) complex of 8h was synthesized, and various spectral, elemental and thermal analysis results confirmed that the central Cr(III) atom coordinated with adjacent hydroxyl groups of two 8h ligands, nitrate and H2O, respectively. (author)

Antagonism in the extraction of uranium(VI) by the binary mixture of PC88A and benzimidazole

International Nuclear Information System (INIS)

Mukherjee, A.; Kamila, S.; Chakravortty, V.

1999-01-01

Extraction studies of uranium(VI) by the binary mixture of PC88A and benzimidazole show an antagonistic behavior in the concentration range 10 -5 -10 -6 M of PC88A and 0.005M of benzimidazole. Antagonism is observed due to the deprotonation of PC88A by benzimidazole forming an adduct resulting in the virtual removal of PC88A from the system. (author)

2-Aryl benzimidazoles: Synthesis, In vitro α-amylase inhibitory activity, and molecular docking study.

Science.gov (United States)

Adegboye, Akande Akinsola; Khan, Khalid Mohammed; Salar, Uzma; Aboaba, Sherifat Adeyinka; Kanwal; Chigurupati, Sridevi; Fatima, Itrat; Taha, Mohammad; Wadood, Abdul; Mohammad, Jahidul Isalm; Khan, Huma; Perveen, Shahnaz

2018-04-25

Despite of many diverse biological activities exhibited by benzimidazole scaffold, it is rarely explored for the α-amylase inhibitory activity. For that purpose, 2-aryl benzimidazole derivatives 1-45 were synthesized and screened for in vitro α-amylase inhibitory activity. Structures of all synthetic compounds were deduced by various spectroscopic techniques. All compounds revealed inhibition potential with IC 50 values of 1.48 ± 0.38-2.99 ± 0.14 μM, when compared to the standard acarbose (IC 50  = 1.46 ± 0.26 μM). Limited SAR suggested that the variation in the inhibitory activities of the compounds are the result of different substitutions on aryl ring. In order to rationalize the binding interactions of most active compounds with the active site of α-amylase enzyme, in silico study was conducted. Copyright © 2018 Elsevier Masson SAS. All rights reserved.

Ionic conducting poly-benzimidazoles

International Nuclear Information System (INIS)

Jouanneau, J.

2006-11-01

Over the last years, many research works have been focused on new clean energy systems. Hydrogen fuel cell seems to be the most promising one. However, the large scale development of this technology is still limited by some key elements. One of them is the polymer electrolyte membrane 'Nafion' currently used, for which the ratio performance/cost is too low. The investigations we carried out during this thesis work are related to a new class of ionic conducting polymer, the sulfonated poly-benzimidazoles (sPBI). Poly-benzimidazoles (PBI) are aromatic heterocyclic polymers well-known for their excellent thermal and chemical stability. Ionic conduction properties are obtained by having strong acid groups (sulfonic acid SO 3 H) on the macromolecular structure. For that purpose, we first synthesized sulfonated monomers. Their poly-condensation with an appropriate non-sulfonated co-monomer yields to sPBI with sulfonation range from 0 to 100 per cent. Three different sPBI structures were obtained, and verified by appropriate analytical techniques. We also showed that the protocol used for the synthesis resulted in high molecular weights polymers. We prepared ionic conducting membrane by casting sPBI solutions on glass plates. Their properties of stability, water swelling and ionic conductivity were investigated. Surprisingly, the behaviour of sPBI was quite different from the other sulfonated aromatic polymers with same amount of SO 3 H, their stability was much higher, but their water swelling and ionic conductivity were quite low. We attributed these differences to strong ionic interactions between the sulfonic acid groups and the basic benzimidazole groups of our polymers. However, we managed to solve this problem synthesizing very highly sulfonated PBI, obtaining membranes with a good balance between all the properties necessary. (author)

Convenient synthesis of benzothiazoles and benzimidazoles through Brønsted acid catalyzed cyclization of 2-amino thiophenols/anilines with β-diketones.

Science.gov (United States)

Mayo, Muhammad Shareef; Yu, Xiaoqiang; Zhou, Xiaoyu; Feng, Xiujuan; Yamamoto, Yoshinori; Bao, Ming

2014-02-07

Brønsted acid catalyzed cyclization reactions of 2-amino thiophenols/anilines with β-diketones under oxidant-, metal-, and radiation-free conditions are described. Various 2-substituted benzothiazoles/benzimidazoles are obtained in satisfactory to excellent yields. Different groups such as methyl, chloro, nitro, and methoxy linked on benzene rings were tolerated under the optimized reaction conditions.

Structure-Activity Relationships of 1,2-Disubstituted Benzimidazoles: Selective Inhibition of Heme Oxygenase-2 Activity.

Science.gov (United States)

Kong, Xianqi; Vukomanovic, Dragic; Nakatsu, Kanji; Szarek, Walter A

2015-08-01

Devising ways to up- or down-regulate heme oxygenase activity is attracting much interest as a strategy for the treatment of a variety of disorders. With a view of obtaining compounds that exhibit high potency and selectivity as inhibitors of the heme oxygenase-2 (HO-2) isozyme (constitutive) relative to the heme oxygenase-1 (HO-1) isozyme (inducible), several 1,2-disubstituted 1H-benzimidazoles were designed and synthesized. Specifically, analogues were synthesized in which the C2 substituent was the following: (1H-imidazol-1-yl)methyl, (N-morpholinyl)methyl, cyclopentylmethyl, cyclohexylmethyl, or (norborn-2-yl)methyl. Compounds with the cyclic system in the C2 substituent being a carbocyclic ring, especially cyclohexyl or norborn-2-yl, and the N1 substituent being a ring-substituted benzyl group, especially 4-chlorobenzyl or 4-bromobenzyl, best exhibited the target criteria of high potency and selectivity toward inhibition of HO-2. The new candidates should be useful pharmacological tools and may have therapeutic applications. © 2015 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

Seven benzimidazole pesticides combined at sub-threshold levels induce micronuclei in vitro

Science.gov (United States)

Ermler, Sibylle; Scholze, Martin; Kortenkamp, Andreas

2013-01-01

Benzimidazoles act by disrupting microtubule polymerisation and are capable of inducing the formation of micronuclei. Considering the similarities in their mechanisms of action (inhibition of microtubule assembly by binding to the colchicine-binding site on tubulin monomers), combination effects according to the principles of concentration addition might occur. If so, it is to be expected that several benzimidazoles contribute to micronucleus formation even when each single one is present at or below threshold levels. This would have profound implications for risk assessment, but the idea has never been tested rigorously. To fill this gap, we analysed micronucleus frequencies for seven benzimidazoles, including the fungicide benomyl, its metabolite carbendazim, the anthelmintics albendazole, albendazole oxide, flubendazole, mebendazole and oxibendazole. Thiabendazole was also tested but was inactive. We used the cytochalasin-blocked micronucleus assay with CHO-K1 cells according to OECD guidelines, and employed an automated micronucleus scoring system based on image analysis to establish quantitative concentration–response relationships for the seven active benzimidazoles. Based on this information, we predicted additive combination effects for a mixture of the seven benzimidazoles by using the concepts of concentration addition and independent action. The observed effects of the mixture agreed very well with those predicted by concentration addition. Independent action underestimated the observed combined effects by a large margin. With a mixture that combined all benzimidazoles at their estimated threshold concentrations for micronucleus induction, micronucleus frequencies of ~15.5% were observed, correctly anticipated by concentration addition. On the basis of independent action, this mixture was expected to produce no effects. Our data provide convincing evidence that concentration addition is applicable to combinations of benzimidazoles that form micronuclei

Benzimidazoles Pharmacodynamics in Equine Strongyles

Directory of Open Access Journals (Sweden)

Laura Catana

2016-11-01

Full Text Available Our research aimed to assess the effectiveness of four benzimidazoles: albendazole, fenbendazole, mebendazole and thiabendazole against equine strongyles. The tests were performed between March 2015 and May 2016, on samples collected from 20 horses and 8 donkeys living in Harghita County. In vivo, Faecal Egg Count Reduction Test (FECRT was used to evaluate fenbendazole pharmacodynamics. In vitro, Egg hatch assay (EHA and Larval development assay (LDA were used to evaluate the effectiveness of albendazole, fenbendazole, mebendazole and thiabendazole. The predominance of small strongyle species was observed, mostly Cyathostomum type A. In the horse group, before treatment, the average intensity was 1595.5 EPG, the maximum value being 4000, and extensivity 55%. Tested again at 14 days after treatment, all samples were negative. In the donkey group, before treatment, the total number was 6550 EPG, intensity of 935.7 and extensivity of 87.5%. 14 days after treatment, the average intensity was 150 and the extensivity 50%. In the horse group, EHA proved the efficacy of fenbendazole (0.0192%, albendazole (0.3740% and thiabendazole (11.62% and a major risk of inducing adaptive phenomena for mebendazole (Y parameter 1009.92. In the donkey group, all benzimidazoles had limited effectiveness: thiabendazole (73.93%, mebendazole (87.51%, fenbendazole (94.05%, albendazole (111.67%. All benzimidazoles inhibited larval development. For all tested benzimidazoles, the resistance induction predictive comparative risk analysis highlighted the benefit of their use, provided that the treatment protocol allows sufficient contact time.

Study of the 14C benzimidazole distribution in mice after inter-peritoneal injection

International Nuclear Information System (INIS)

Tyortyalian, C.

1965-01-01

In order to provide further information on the mechanism of benzimidazole radioprotective activity, this work studies the tissual repartition in mice of this compound labelled with carbon 14. Experiments have showed that benzimidazole distribution is fast and homogeneous in all the tissues, but however affinity appears at the level of stomach and gastric content. Elimination is made through the urinary system and is very fast. (author) [fr

Multifunctional Poly(2,5-benzimidazole)/Carbon Nanotube Composite Films

Science.gov (United States)

2010-01-01

Multifunctional Poly(2,5- benzimidazole )/Carbon Nanotube Composite Films JI-YE KANG,1 SOO-MI EO,1 IN-YUP JEON,1 YEONG SUK CHOI,2 LOON-SENG TAN,3 JONG...molecular-weight poly(2,5- benzimidazole ) (ABPBI). ABPBI/carbon nanotube (CNT) compo- sites were prepared via in situ polymerization of the AB-monomer in the...polymerization; multiwalled carbon nanotube (MWCNT); nano- composites; poly(2,5- benzimidazole ); (ABPBI); polycondensa- tion; poly(phosphoric acid); single-walled

Comprehensive Review in Current Developments of Benzimidazole-Based Medicinal Chemistry.

Science.gov (United States)

Keri, Rangappa S; Hiremathad, Asha; Budagumpi, Srinivasa; Nagaraja, Bhari Mallanna

2015-07-01

The properties of benzimidazole and its derivatives have been studied over more than one hundred years. Benzimidazole derivatives are useful intermediates/subunits for the development of molecules of pharmaceutical or biological interest. Substituted benzimidazole derivatives have found applications in diverse therapeutic areas such as antiulcer, anticancer agents, and anthelmintic species to name just a few. This work systematically gives a comprehensive review in current developments of benzimidazole-based compounds in the whole range of medicinal chemistry as anticancer, antibacterial, antifungal, anti-inflammatory, analgesic agents, anti-HIV, antioxidant, anticonvulsant, antitubercular, antidiabetic, antileishmanial, antihistaminic, antimalarial agents, and other medicinal agents. This review will further be helpful for the researcher on the basis of substitution pattern around the nucleus with an aim to help medicinal chemists for developing an SAR on benzimidazole drugs/compounds. © 2014 John Wiley & Sons A/S.

An efficient one-pot two catalyst system in the construction of 2-substituted benzimidazoles: synthesis of benzimidazo[1,2-c]quinazolines.

Science.gov (United States)

Cimarelli, Cristina; Di Nicola, Matteo; Diomedi, Simone; Giovannini, Riccardo; Hamprecht, Dieter; Properzi, Roberta; Sorana, Federico; Marcantoni, Enrico

2015-12-28

The benzimidazole core is a common moiety in a large number of natural products and pharmacologically active small molecules. The synthesis of novel benzimidazole derivatives remains a main focus in medicinal research. In continuation of the efforts towards Ce(III) catalysts for organic transformations, we observed for the first time the activity of the iodide ion and copper cation in activating CeCl3·7H2O in the selective formation of prototypical 2-substituted benzimidazoles. The one-pot CeCl3·7H2O-CuI catalytic system procedure includes the cyclo-dehydrogenation of aniline Schiff's bases, generated in situ from the condensation of 1,2-phenylenediamine and aldehydes, followed by the oxidation with iodine, which works as a hydrogen sponge. Mild reaction conditions, good to excellent yields, and clean reactions make the procedure a useful contribution to the synthesis of biologically active fused heterocycles containing benzimidazoquinazolines.

Benzimidazole as Novel Therapy for Hormone-Refractory Metastatic Prostate Cancer

Science.gov (United States)

2011-05-01

8 4 INTRODUCTION The focus of this project is to evaluate the anti-tumor effects of benzimidazoles as a...potential anti-metastatic prostate cancer therapy. We identified benzimidazoles , a class of anti-parasitic drug, in a drug screening process for...preferential anti-tumor activity on metastatic prostate cancer cells. We have data indicate that benzimidazoles have potent anti-tumor activities

SYNTHESIS, SPECTRAL AND THEORETICAL CHARACTERIZATION OF 5,6-DICHLORO/DIMETHYL-2-(2´,3´/2´,4´/2´,5´/3´,4´/3´,5´-DIMETHOXYPHENYL-1H-BENZIMIDAZOLES

Directory of Open Access Journals (Sweden)

Demet Gürbüz

2016-12-01

Full Text Available 5,6-Dichloro/dimethyl-2-(2´,3´/2´,4´/2´,5´/3´,4´/3´,5´-dimethoxyphenyl-1H-benzimidazoles were synthesized and characterized by using analytical data, FT-IR, FT-Raman, NMR, ESI-MS and fl uorescence spectroscopy. The optimized molecular geometry, zero point energy, dipole moment, ESE, band gap and charge distributions were calculated by Gaussian 09 using Density Functional Theory (DFT, RB3LYP with 6-31++G(d,p basis set. According to the calculations, the molecules have structures with various torsion angles between the benzimidazole and benzene rings from 9.7º to 47.8º. The calculated energy values with ZPE correction and DFT show that the methyl derivatives are more stable than the chloro forms. 3´,4´-Dimethoxy derivatives have higher decomposition points in comparison with the other compounds in series. The chlorine atoms of 5,6-dichloro-2- (2´,3´/2´,4´/2´,5´/3´,4´/3´,5´-dimethoxyphenyl-1H-benzimidazoles are positively charged whereas the C5 and C6 carbon atoms are negatively charged due to the attached chlorine atoms, in virtue of the electron withdrawing characteristic of the imidazole part of the benzimidazole ring. Also, some calculated prominent bond lengths and bond angles were discussed.

Antiprotozoal activities of benzimidazoles and correlations with beta-tubulin sequence.

Science.gov (United States)

Katiyar, S K; Gordon, V R; McLaughlin, G L; Edlind, T D

1994-01-01

Benzimidazoles have been widely used since the 1960s as anthelmintic agents in veterinary and human medicine and as antifungal agents in agriculture. More recently, selected benzimidazole derivatives were shown to be active in vitro against two protozoan parasites, Trichomonas vaginalis and Giardia lamblia, and clinical studies with AIDS patients have suggested that microsporidia are susceptible as well. Here, we first present in vitro susceptibility data for T. vaginalis and G. lamblia using an expanded set of benzimidazole derivatives. Both parasites were highly susceptible to four derivatives, including mebendazole, flubendazole, and fenbendazole (50% inhibitory concentrations of 0.005 to 0.16 microgram/ml). These derivatives also had lethal activity that was time dependent: 90% of T. vaginalis cells failed to recover following a 20-h exposure to mebendazole at 0.17 microgram/ml. G. lamblia, but not T. vaginalis, was highly susceptible to five additional derivatives. Next, we examined in vitro activity of benzimidazoles against additional protozoan parasites: little or no activity was observed against Entamoeba histolytica, Leishmania major, and Acanthamoeba polyphaga. Since the microtubule protein beta-tubulin has been identified as the benzimidazole target in helminths and fungi, potential correlations between benzimidazole activity and beta-tubulin sequence were examined. This analysis included partial sequences (residues 108 to 259) from the organisms mentioned above, as well as the microsporidia Encephalitozoon hellem and Encephalitozoon cuniculi and the sporozoan Cryptosporidium parvum. beta-tubulin residues Glu-198 and, in particular, Phe-200 are strong predictors of benzimidazole susceptibility; both are present in Encephalitozoon spp. but absent in C. parvum. PMID:7811023

Synthesis of benzimidazoles via iridium-catalyzed acceptorless dehydrogenative coupling.

Science.gov (United States)

Sun, Xiang; Lv, Xiao-Hui; Ye, Lin-Miao; Hu, Yu; Chen, Yan-Yan; Zhang, Xue-Jing; Yan, Ming

2015-07-21

Iridium-catalyzed acceptorless dehydrogenative coupling of tertiary amines and arylamines has been developed. A number of benzimidazoles were prepared in good yields. An iridium-mediated C-H activation mechanism is suggested. This finding represents a novel strategy for the synthesis of benzimidazoles.

Transition-metal-free synthesis of imidazo[2,1-b]thiazoles and thiazolo[3,2-a]benzimidazoles via an S-propargylation/5-exo-dig cyclization/isomerization sequence using propargyl tosylates as substrates.

Science.gov (United States)

Omar, Mohamed A; Frey, Wolfgang; Conrad, Jürgen; Beifuss, Uwe

2014-11-07

A transition-metal-free route for the synthesis of several N-fused heterocycles, including thiazolo[3,2-a]benzimidazoles and imidazo[2,1-b]thiazoles, is reported. The reaction between propargyl tosylates and 2-mercaptobenzimidazoles under basic conditions results in 3-substituted thiazolo[3,2-a]benzimidazoles, in yields up to 92% in a single synthesis step. With 2-mercaptoimidazoles as the substrate, the corresponding imidazo[2,1-b]thiazoles were exclusively obtained. The transformation is considered to proceed as an intermolecular S-propargylation that is followed by 5-exo-dig ring closure and double-bond isomerization.

Crystal structures of eight 3D molecular adducts derived from bis-imidazole, bis(benzimidazole), and organic acids

Science.gov (United States)

Ding, Aihua; Jin, Shouwen; Jin, Shide; Hu, KaiKai; Lin, Zhihao; Liu, Hui; Wang, Daqi

2018-01-01

Cocrystallization of the bis(imidazole)/bis(benzimidazole) with a series of organic acids gave a total of eight molecular adducts with the compositions: (3,6-bis(imidazole-1-yl)pyridazine): (trichloroacetic acid)2(1) [(H2L1)2+ · (tca-)2, L1 = 3,6-bis(imidazole-1-yl)pyridazine, tca- = trichloroacetate], (bis(N-imidazolyl)methane): (suberic acid) (2) [(L2) · (H2suba), L2 = bis(N-imidazolyl)methane, H2suba = suberic acid], bis(N-imidazolyl)methane: (3-nitrophthalic acid): 3H2O (3) [(H2L2)2+ · (3-Hnpa-)2 · 3H2O, 3-Hnpa- = 3-nitro hydrogenphthalate], (bis(N-imidazolyl)butane)0.5: (4-nitrophthalic acid): H2O (4) [(H2L3)0.5+ · (4-Hnpa-)- · H2O, L3 = bis(N-imidazolyl)butane, 4-Hnpa- = 4-nitro hydrogenphthalate], (1-(3-(1H-benzimidazol-1-yl)propyl)-1H-benzimidazole): (3,5-dinitrosalicylic acid) (5) [(HL4) · (3,5-dns-), L4 = 1-(3-(1H-benzimidazol-1-yl)propyl)-1H-benzimidazole, 3,5-dns- = 3,5-dinitrosalicylate], (1-(3-(1H-benzimidazol-1-yl)propyl)-1H-benzimidazole): (3-nitrophthalic acid) (6) [(H2L4) · (3-npa2-), L4 = 1-(3-(1H-benzimidazol-1-yl)propyl)-1H-benzimidazole, 3-npa2-=3-nitrogenphthalate], (bis(N-imidazolyl)butane): (pamoic acid) (7) [(H2L3) · (pam), pam = pamoate], and (3,6-bis(imidazole-1-yl)pyridazine): (1,5-naphthalenedisulfonic acid) [(H2L1)2+ · (npda)2- = 1,5-naphthalenedisulfonate] (8). The eight adducts have been characterized by X-ray diffraction technique, infrared spectrum, and elemental analysis, and the melting points of all adducts were also reported. And their structural and supramolecular aspects are fully analyzed. The result reveals that among the eight investigated crystals both the end ring N in the bis(imidazole) moieties are protonated when the organic acids are deprotonated except 2, and 5, and the crystal packing is interpreted in terms of the strong ionic Nsbnd H⋯O H-bond between the imidazolium and the deprotonated acidic groups. Except the Nsbnd H⋯O H-bond, the Osbnd H⋯O H-bonds were also found at the salts 3, 4

Process design of high-concentration benzimidazole wastewater treatment based on the molecular structure of contaminants.

Science.gov (United States)

Li, Chenru; Qian, Kun; Liu, Qinyao; Zhang, Qianyi; Yao, Chen; Song, Wei; Wang, Yihong

2018-04-01

Benzimidazole is an important intermediate in industry and it is usually difficult to be degraded by many treatment technologies. Looking for a highly effective, environment-friendly degradation process for benzimidazole wastewater is of great significance to reduce pollution. Based on the structure of contaminants, the micro-electrolysis (ME) coupled with the Fenton technique was chosen to degrade the industrial benzimidazole wastewater. Special feeding was applied to maintain the suitable hydrogen peroxide (H 2 O 2 ) concentration to produce the hydroxyl radicals (•OH) as much as possible and protect •OH from being quenched by excess H 2 O 2 according to the reaction mechanism. The results showed that this combined technique was highly efficient to decompose benzimidazole compounds. More chemical oxygen demand (COD) could be reduced when flow control was used, compared to the flow not being controlled. The COD removal rate could reach 85.2% at optimal parameters. Then the effluent of this process was combined with the existing biochemical system for further degradation. The studies of Ultraviolet Spectrophotometry, Fourier Transform Infrared Spectroscopy and Liquid Chromatography Mass Spectrometry showed that both 2-(a-Hydroxyethyl) benzimidazole and 2-Acetylbenzimidazole were decomposed to the isopropanolamine and aniline after the ME treatment; then the intermediates were oxidized into oxalic acid after the Fenton reaction.

DFT and electrochemical studies of tris(benzimidazole-2-ylmethyl)amine as an efficient corrosion inhibitor for carbon steel surface

Energy Technology Data Exchange (ETDEWEB)

Roque, Jacinto Morales [Facultad de Quimica, Universidad Nacional Autonoma de Mexico, Mexico D.F. 04510 (Mexico); Pandiyan, T. [Facultad de Quimica, Universidad Nacional Autonoma de Mexico, Mexico D.F. 04510 (Mexico)], E-mail: pandiyan@servidor.unam.mx; Cruz, J. [Centro de Investigaciones Quimicas, Universidad Autonoma del Estado de Hidalgo, Unidad Universitaria, Km 4.5 Carretera Pachuca-Tulancingo, C.P. 42184 Pachuca-Hidalgo (Mexico); Garcia-Ochoa, E. [Centro de Investigacion en Corrosion, Universidad Autonoma de Campeche, Mexico, Av. Agustin Melgar s/n, Colonia Buenavista, San Francisco de Campeche, Cam. C.P. 24030 (Mexico)

2008-03-15

The corrosion inhibition properties of tris(benzimidazole-2-ylmethyl)amine (TBMA) were analyzed by DFT and electrochemical techniques such as polarization curves and electrochemical impedance spectroscopy (EIS). DFT results clearly show that TBMA posses corrosion inhibition properties by having a delocalization region (N{sub 1}=C{sub 2}=N{sub 3}) in the benzimidazole ring that gives up their {pi} electron density through its HOMO orbital to the metal LUMO to form a adsorption layer over the metallic surface; this has been proved by interacting the TBMA and its protonated structures with the surface of Fe{sub 13} cluster, showing that the protonated moiety adsorbs strongly on the iron surface than that of the neutral structure. Electrochemical impedance data demonstrate that the interface between the electrode and the TBMA solution decreases the charge capacitance and simultaneously increases the function of the charge/discharge of the interface, facilitating the formation of adsorption layer over the iron surface.

DFT and electrochemical studies of tris(benzimidazole-2-ylmethyl)amine as an efficient corrosion inhibitor for carbon steel surface

International Nuclear Information System (INIS)

Roque, Jacinto Morales; Pandiyan, T.; Cruz, J.; Garcia-Ochoa, E.

2008-01-01

The corrosion inhibition properties of tris(benzimidazole-2-ylmethyl)amine (TBMA) were analyzed by DFT and electrochemical techniques such as polarization curves and electrochemical impedance spectroscopy (EIS). DFT results clearly show that TBMA posses corrosion inhibition properties by having a delocalization region (N 1 =C 2 =N 3 ) in the benzimidazole ring that gives up their π electron density through its HOMO orbital to the metal LUMO to form a adsorption layer over the metallic surface; this has been proved by interacting the TBMA and its protonated structures with the surface of Fe 13 cluster, showing that the protonated moiety adsorbs strongly on the iron surface than that of the neutral structure. Electrochemical impedance data demonstrate that the interface between the electrode and the TBMA solution decreases the charge capacitance and simultaneously increases the function of the charge/discharge of the interface, facilitating the formation of adsorption layer over the iron surface

Dioxouranium(VI) complexes with benzimidazole and benzoxazole derivatives

International Nuclear Information System (INIS)

Mansingh, P.S.; Dash, K.C.

1995-01-01

UO 2 LηX 2 [X = NO 3 ,NCS and 0.5 SO 4 and when n = 2, L = 2-(2-hydroxyphyenyl) benzimidazole (HPBI) or 2-(2-aminophenyl) benzimidazole(APBI) and for n=1, L = 2-(2-pyridyl) benzoxazole (PBO)] were synthesized and characterized by several physico chemical techniques including molar conductance data, IR, 1 H and 13 C NMR and thermogravimetric analysis. (author). 5 refs

Benzimidazole-loaded Halloysite Nanotube as a Smart Coating Application

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Khairina Azmi Zahidah

2017-09-01

Full Text Available Smart coating has been developed for the corrosion control of surfaces exposed to corrosive environment. An important step in development of a smart coating is the successful impregnation of corrosion inhibitor into the nanocontainer as a coating pigment. In this study, halloysite was used as nanocontainer to encapsulate benzimidazole as corrosion inhibitor by vacuum method. FESEM, TEM, FTIR and TGA characterization techniques were used to confirm the loading of halloysite with benzimidazole. FESEM results indicated differences between the morphology of the unloaded-halloysite and benzimidazole loaded-halloysite. TEM results confirmed that benzimidazole molecules are loaded into halloysite. FTIR result revealed there are differences in the absorbance characteristic of peaks between peak number 1000-4000 cm-1 for loaded and unloaded samples. It is seen that the absorbance in the loaded-halloysite is higher than unloaded-halloysite, which confirms quantity/specific functional group of molecules. TGA result showed the temperature of degradation of benzimidazole-loaded HNT was higher than pure HNT. EIS was conducted to examine the protection characteristic of the developed smart coating. From EIS results, of 1, 3, and 6 days of experimental duration, it is seen that the value of coating impedance (Z’ after exposure to 3.5% NaCl environment is very height, 2.460E+07 Ω, which confirm a very good anti corrosion protection characteristic for the developed smart coating. 

Synthesis and Analgesic Activity of Novel Derivatives of 1,2-Substituted Benzimidazoles

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Shobhit Srivastava

2013-01-01

Full Text Available A series of novel 2-phenylhydrazinomethyl and 2-(2-hydroxyphenyl-benzimidazole derivatives substituted at the N1-position of benzimidazole nucleus were synthesized as well as screened for analgesic activity. Some of these compounds showed promising analgesic activity when compared with the standard drug diclofenac sodium. The incorporation of a phenylhydrazinomethyl nucleus at 2-position of benzimidazole compound gave a biologically active pharmacophore.

Iminodiacetic acid derivatives of benzimidazole. Synthesis of N-(benzimidazol-2-ylmethyl)iminodiacetic acids

Energy Technology Data Exchange (ETDEWEB)

Hunt, F C; Wilson, J G [Australian Atomic Energy Commission Research Establishment, Lucas Heights. Isotope Div.

1983-01-01

Ten new N-(2-benzimidazolylmethyl)iminodiacetic acids (BIMIDA) have been synthesized from the corresponding o-phenylenediamines via intermediate 2-chloromethyl and 2-aminomethyl benzimidazoles as ligands for Tc-99m. Anomalies associated with the synthesis of the iodo-substituted compound are described.

Potential radiosensitizing agents. 5. 2-Substituted benzimidazole derivatives

International Nuclear Information System (INIS)

Gupta, R.P.; Larroquette, C.A.; Agrawal, K.C.

1982-01-01

A series of 2-substituted benzimidazoles and their derivatives have been synthesized and tested for their ability to selectively sensitize hypoxic Chinese hamster cells (V-79) toward the lethal effect of ionizing radiation. These compounds were prepared by reacting the 2-substituted benzimidazoles with 1,2-epoxy-3-methoxypropane in the presence of potassium carbonate. Reaction of the 2-nitro and 2-methylfonyl analogue with the epoxide also yielded a cyclized material, which was confirmed to be a benzimidazo[2,1-b]oxazole. In an attempt to increase the electron affinity, 5- or 6-nitro-2-substituted-benzimidazoles were also synthesized and then reacted with the epoxide to yield the corresponding 1-substituted derivatives. The results of the biological tests for the radiosensitizing activity of these agents against Chinese hamster cells (V-79) in culture indicated that the 2-nitro-substituted analogues were the most effective sensitizers in this series

ring system

African Journals Online (AJOL)

1,3,2-DIAZABORACYCLOALKANE. RING SYSTEM. Negussie Retta" and Robert H. Neilson. 'Department of Chemistry, Addis Ababa University, P.O. Box 1176, Addis Ababa, Ethiopia. Department of Chemistry, Texas Christian University.

Methyl 2-Benzamido-2-(1H-benzimidazol-1-ylmethoxyacetate

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Alami Anouar

2012-09-01

Full Text Available The heterocyclic carboxylic α-aminoester methyl 2-benzamido-2-(1H-benzimidazol-1-ylmethoxyacetate is obtained by O-alkylation of methyl α-azido glycinate N-benzoylated with 1H-benzimidazol-1-ylmethanol.

Rhenium(V) complexing with benzimidazole in acidic media

International Nuclear Information System (INIS)

Zakaeva, R.Sh.; Gagieva, S.Ch.; Kaloev, N.I.; Bukov, N.N.; Panyushkin, V.T.

2003-01-01

Coordination compounds of rhenium(V) with 1H-benzimidazole (L) separated from acid media: (HL) 2 [ReOX 5 ](H 2 O) n and [ReOL x X y (H 2 O) z ](H 2 O) n (HL and L - protonated and deprotonated forms of benzimidazole; X = Cl - , Br - ) were studied by the methods of IR spectroscopy, 1 H NMR spectroscopy and thermal gravimetric analysis. Methods of ligand coordination in the complexes are discussed on the basis of data obtained [ru

Biological Activity and Molecular Structures of Bis(benzimidazole and Trithiocyanurate Complexes

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Pavel Kopel

2015-06-01

Full Text Available 1-(1H-Benzimidazol-2-yl-N-(1H-benzimidazol-2-ylmethylmethanamine (abb and 2-(1H-benzimidazol-2-ylmethylsulfanylmethyl-1H-benzimidazole (tbb have been prepared and characterized by elemental analysis. These bis(benzimidazoles have been further used in combination with trithiocyanuric acid for the preparation of complexes. The crystal and molecular structures of two of them have been solved. Each nickel atom in the structure of trinuclear complex [Ni3(abb3(H2O3(μ-ttc](ClO43·3H2O·EtOH (1, where ttcH3 = trithiocyanuric acid, is coordinated with three N atoms of abb, the N,S donor set of ttc anion and an oxygen of a water molecule. The crystal of [(tbbH2(ttcH22(ttcH3(H2O] (2 is composed of a protonated bis(benzimidazole, two ttcH2 anions, ttcH3 and water. The structure is stabilized by a network of hydrogen bonds. These compounds were primarily synthesized for their potential antimicrobial activity and hence their possible use in the treatment of infections caused by bacteria or yeasts (fungi. The antimicrobial and antifungal activity of the prepared compounds have been evaluated on a wide spectrum of bacterial and yeast strains and clinical specimens isolated from patients with infectious wounds and the best antimicrobial properties were observed in strains after the use of ligand abb and complex 1, when at least 80% growth inhibition was achieved.

In Situ formation of pentafluorophosphate benzimidazole anion stabilizes high-temperature performance of lithium-ion batteries

International Nuclear Information System (INIS)

Pradanawati, Sylvia Ayu; Wang, Fu-Ming; Rick, John

2014-01-01

Highlights: • A new pentafluorophosphate benzimidazole anion was formed by Lewis acid-base reaction. • This pentafluorophosphate benzimidazole anion is fabricated with the benzimidazole anion and PF 5 . • This pentafluorophosphate benzimidazole anion avoids the ominous side reactions that PF 5 reacts SEI to form LiF and HF at high temperature. • The additional pentafluorophosphate benzimidazole anion formation well maintains the battery performance at 60 °C measurement compares to the electrolyte only with contains the salt, LiPF 6 . - Abstract: Lithium salts play a critical role in initiating electrochemical reactions in Li-ion batteries. Single Li ions dissociate from bulk-salt and associate with carbonates to form a solid electrolyte interface (SEI) during the first charge-discharge of the battery. SEI formation and the chemical stability of salt must both be controlled and optimized to minimize irreversible reactions in SEI formation and to suppress the decomposition of the salt at high temperatures. This study synthesizes a new benzimidazole-based anion in the electrolyte. This anion, pentafluorophosphate benzimidazole, results from a Lewis acid-base reaction between the benzimidazole anion and PF 5 . The new pentafluorophosphate benzimidazole anion inhibits the decomposition of LiPF 6 by inhibiting PF 5 side reactions, which degrade the SEI, and lead to the formation of LiF and HF at high temperatures. In addition, the use of the pentafluorophosphate benzimidazole anion results in the formation of a modified SEI that is able to modify the battery's performance. Cyclic voltammetry, scanning electron microscopy, differential scanning calorimetry, electrochemical impedance spectroscopy, as well as charge-discharge and X-ray photoelectron spectroscopy measurements have been used to characterize the materials in this study. The formation of the pentafluorophosphate benzimidazole anion in the electrolyte caused a 14% decrease in the activation energy

Planetary ring systems properties, structures, and evolution

CERN Document Server

Murray, Carl D

2018-01-01

Planetary rings are among the most intriguing structures of our solar system and have fascinated generations of astronomers. Collating emerging knowledge in the field, this volume reviews our current understanding of ring systems with reference to the rings of Saturn, Uranus, Neptune, and more. Written by leading experts, the history of ring research and the basics of ring–particle orbits is followed by a review of the known planetary ring systems. All aspects of ring system science are described in detail, including specific dynamical processes, types of structures, thermal properties and their origins, and investigations using computer simulations and laboratory experiments. The concluding chapters discuss the prospects of future missions to planetary rings, the ways in which ring science informs and is informed by the study of other astrophysical disks, and a perspective on the field's future. Researchers of all levels will benefit from this thorough and engaging presentation.

Microwave-assisted Synthesis of Benzimidazole Derivatives from Citronellal in Kaffir Lime (Citrus hystrix DC.) Oil

Science.gov (United States)

Sapri Ramadhan, Dwi; Warsito; Dhiaul Iftitah, Elvina

2018-01-01

Benzimidazoles are an important group of heterocyclic aromatic organic compound in the field of medicinal chemistry. It plays a very important role in pharmacological activity such as, analgesic, antiinflammatory, antibacterial, anti ungal, anti iral, antithelmenthic, anti convulsant, antihypertensive, and antiulcer. The synthesis of benzimidazole derivative under microwave irradiation of citronellal as raw material which is extracted from Citrus hystrix DC. (kaffir lime) leaves. The reaction using methanol and dichloromethane as solvent with variation of reaction time at 30, 40, 50, 60, and 70 minutes and mole ratio of citronellal to 1,2-phenylenediamine, 1:1, 1:1.5, and 1:2, respectively. Synthesis products was characterized by FT-IR and GC-MS. The optimum reaction time was obtained at 60 minutes in the present of dichloromethane and 1:2 mole ratio of citronellal to 1,2-phenylenediamine. The yield of the product is 42.19%. Structure of the synthesized compound were assigned on spectrum bands for C=N str at 1661 cm-1, C-N str at 1271 cm-1, C=C str of benzene ring at 1622 and 1456 cm-1 and C=C str of alkene at 1379 cm-1. GC-MS analysis showed single peak with retention time of 15.339 minute and m/z 242.

Discovery of genomic intervals that underlie nematode responses to benzimidazoles.

Science.gov (United States)

Zamanian, Mostafa; Cook, Daniel E; Zdraljevic, Stefan; Brady, Shannon C; Lee, Daehan; Lee, Junho; Andersen, Erik C

2018-03-01

Parasitic nematodes impose a debilitating health and economic burden across much of the world. Nematode resistance to anthelmintic drugs threatens parasite control efforts in both human and veterinary medicine. Despite this threat, the genetic landscape of potential resistance mechanisms to these critical drugs remains largely unexplored. Here, we exploit natural variation in the model nematodes Caenorhabditis elegans and Caenorhabditis briggsae to discover quantitative trait loci (QTL) that control sensitivity to benzimidazoles widely used in human and animal medicine. High-throughput phenotyping of albendazole, fenbendazole, mebendazole, and thiabendazole responses in panels of recombinant lines led to the discovery of over 15 QTL in C. elegans and four QTL in C. briggsae associated with divergent responses to these anthelmintics. Many of these QTL are conserved across benzimidazole derivatives, but others show drug and dose specificity. We used near-isogenic lines to recapitulate and narrow the C. elegans albendazole QTL of largest effect and identified candidate variants correlated with the resistance phenotype. These QTL do not overlap with known benzimidazole target resistance genes from parasitic nematodes and present specific new leads for the discovery of novel mechanisms of nematode benzimidazole resistance. Analyses of orthologous genes reveal conservation of candidate benzimidazole resistance genes in medically important parasitic nematodes. These data provide a basis for extending these approaches to other anthelmintic drug classes and a pathway towards validating new markers for anthelmintic resistance that can be deployed to improve parasite disease control.

Ionic conducting poly-benzimidazoles; Polybenzimidazoles conducteurs ioniques

Energy Technology Data Exchange (ETDEWEB)

Jouanneau, J

2006-11-15

Over the last years, many research works have been focused on new clean energy systems. Hydrogen fuel cell seems to be the most promising one. However, the large scale development of this technology is still limited by some key elements. One of them is the polymer electrolyte membrane 'Nafion' currently used, for which the ratio performance/cost is too low. The investigations we carried out during this thesis work are related to a new class of ionic conducting polymer, the sulfonated poly-benzimidazoles (sPBI). Poly-benzimidazoles (PBI) are aromatic heterocyclic polymers well-known for their excellent thermal and chemical stability. Ionic conduction properties are obtained by having strong acid groups (sulfonic acid SO{sub 3}H) on the macromolecular structure. For that purpose, we first synthesized sulfonated monomers. Their poly-condensation with an appropriate non-sulfonated co-monomer yields to sPBI with sulfonation range from 0 to 100 per cent. Three different sPBI structures were obtained, and verified by appropriate analytical techniques. We also showed that the protocol used for the synthesis resulted in high molecular weights polymers. We prepared ionic conducting membrane by casting sPBI solutions on glass plates. Their properties of stability, water swelling and ionic conductivity were investigated. Surprisingly, the behaviour of sPBI was quite different from the other sulfonated aromatic polymers with same amount of SO{sub 3}H, their stability was much higher, but their water swelling and ionic conductivity were quite low. We attributed these differences to strong ionic interactions between the sulfonic acid groups and the basic benzimidazole groups of our polymers. However, we managed to solve this problem synthesizing very highly sulfonated PBI, obtaining membranes with a good balance between all the properties necessary. (author)

Thermostability and photophysical properties of mixed-ligand carboxylate/benzimidazole Zn(II)-coordination polymers

International Nuclear Information System (INIS)

Barros, Bráulio Silva; Chojnacki, Jaroslaw; Macêdo Soares, Antonia Alice; Kulesza, Joanna; Lourenço da Luz, Leonis; Júnior, Severino Alves

2015-01-01

The reaction between Zn(NO 3 ) 2 ·6H 2 O or Zn(CH 3 COO) 2 ·2H 2 O and isophthalic acid (1,3-H 2 bdc) in the presence of benzimidazole (Hbzim) in dimethylformamide (DMF)/ethanol (EtOH)/H 2 O solvent mixture at room temperature yielded two structurally different coordination polymers: [Zn 2 (1,3-bdc) 2 (Hbzim) 2 ] (1) and [Zn 2 (1,3-bdc)(bzim) 2 ] (2). (1) is a 2D-layered framework with a molecule of benzimidazole coordinated to the Zn center, whereas (2) is a 3D framework with benzimidazolate species acting as a co-ligand and bridging two Zn(II) ions. Reactions performed at 90 °C led to the formation of coordination polymers structurally similar to (2), independently of the Zn(II) source used. In the absence of benzimidazole, the reaction between ZnAc 2 .2H 2 O and 1,3-H 2 bdc at 90 °C resulted in the formation of (3), a 3D coordination polymer Zn(HCOO) 3 (Me 2 NH 2 + ). It was observed that the thermostability and the photophysical properties of (1) and (2) are strongly dependent on the coordination modes and packing of benzimidazole in the solid state. These materials present photoluminescence in the wide range of the spectrum, from UV to IR. A full understanding of a physical process occurring in these intriguing systems, including complete energy level diagrams with possible transitions were provided. - Graphical abstract: Display Omitted - Highlights: • Structurally different Zn(II)-coordination polymers were prepared. • The formation of frameworks was counter anion and temperature dependent. • Photoluminescence in the wide range of the spectrum, from UV to IR was observed. • Thermostability and luminescence depended on bzim packing in the structure

Glutathione transferase-mediated benzimidazole-resistance in Fusarium graminearum.

Science.gov (United States)

Sevastos, A; Labrou, N E; Flouri, F; Malandrakis, A

2017-09-01

Fusarium graminearum laboratory mutants moderately (MR) and highly (HR) benzimidazole-resistant, carrying or not target-site mutations at the β 2 -tubulin gene were utilized in an attempt to elucidate the biochemical mechanism(s) underlying the unique BZM-resistance paradigm of this fungal plant pathogen. Relative expression analysis in the presence or absence of carbendazim (methyl-2-benzimidazole carbamate) using a quantitative Real Time qPCR (RT-qPCR) revealed differences between resistant and the wild-type parental strain although no differences in expression levels of either β 1 - or β 2 -tubulin homologue genes were able to fully account for two of the highly resistant phenotypes. Glutathione transferase (GST)-mediated detoxification was shown to be -at least partly- responsible for the elevated resistance levels of a HR isolate bearing the β 2 -tubulin Phe200Tyr resistance mutation compared with another MR isolate carrying the same mutation. This benzimidazole-resistance mechanism is reported for the first time in F. graminearum. No indications of detoxification involved in benzimidazole resistance were found for the rest of the isolates as revealed by GST and glutathione peroxidase (GPx) activities and bioassays using monoxygenase and hydrolase detoxification enzyme inhibiting synergists. Interestingly, besides the Phe200Tyr mutation-carrying HR isolate, the remaining highly-carbendazim resistant phenotypes could not be associated with any of the target site modification/overproduction, detoxification or reduced uptake-increased efflux mechanisms. Copyright © 2016 Elsevier B.V. All rights reserved.

C2-Selective Branched Alkylation of Benzimidazoles by Rhodium(I)-Catalyzed C-H Activation.

Science.gov (United States)

Tran, Gaël; Confair, Danielle; Hesp, Kevin D; Mascitti, Vincent; Ellman, Jonathan A

2017-09-01

Herein, we report a Rh(I)/bisphosphine/K 3 PO 4 catalytic system allowing for the first time the selective branched C-H alkylation of benzimidazoles with Michael acceptors. Branched alkylation with N,N-dimethyl acrylamide was successfully applied to the alkylation of a broad range of benzimidazoles incorporating a variety of N-substituents and with both electron-rich and -poor functionality displayed at different sites of the arene. Moreover, the introduction of a quaternary carbon was achieved by alkylation with ethyl methacrylate. The method was also shown to be applicable to the C2-selective branched alkylation of azabenzimidazoles.

Evidence for Quantisation in Planetary Ring Systems

OpenAIRE

WAYTE, RICHARD

2017-01-01

Absolute radial positions of the main features in Saturn's ring system have been calculated by adapting the quantum theory of atomic spectra. Fine rings superimposed upon broad rings are found to be covered by a harmonic series of the form N α A(r)1/2, where N and A are integers. Fourier analysis of the ring system shows that the spectral amplitude fits a response profile which is characteristic of a resonant system. Rings of Jupiter, Uranus and Neptune also obey the same rules. Involvement o...

A bioassay for the detection of benzimidazoles reveals their presence in a range of environmental samples

Directory of Open Access Journals (Sweden)

Terence S Crofts

2014-11-01

Full Text Available Cobamides are a family of enzyme cofactors that include vitamin B12 (cobalamin and are produced solely by prokaryotes. Structural variability in the lower axial ligand has been observed in cobamides produced by diverse organisms. Of the three classes of lower ligands, the benzimidazoles are uniquely found in cobamides, whereas the purine and phenolic bases have additional biological functions. Many organisms acquire cobamides by salvaging and remodeling cobamides or their precursors from the environment. These processes require free benzimidazoles for incorporation as lower ligands, though the presence of benzimidazoles in the environment has not been previously investigated. Here, we report a new purification method and bioassay to measure the total free benzimidazole content of samples from microbial communities and laboratory media components. The bioassay relies on the calcofluor-bright phenotype of a bluB mutant of the model cobalamin-producing bacterium Sinorhizobium meliloti. The concentrations of individual benzimidazoles in these samples were measured by liquid chromatography-tandem mass spectrometry. Several benzimidazoles were detected in subpicomolar to subnanomolar concentrations in host-associated and environmental samples. In addition, benzimidazoles were found to be common contaminants of laboratory media components. These results suggest that benzimidazoles present in the environment and in laboratory media have the potential to influence microbial metabolic activities.

α-Amino Acid Derived Benzimidazole-Linked Rhodamines: A Case of Substitution Effect at the Amino Acid Site toward Spiro Ring Opening for Selective Sensing of Al3+ Ions.

Science.gov (United States)

Majumdar, Anupam; Mondal, Subhendu; Daniliuc, Constantin G; Sahu, Debashis; Ganguly, Bishwajit; Ghosh, Sourav; Ghosh, Utpal; Ghosh, Kumaresh

2017-08-07

α-Amino acid derived benzimidazole-linked rhodamines have been synthesized, and their metal ion sensing properties have been evaluated. Experimentally, l-valine- and l-phenylglycine-derived benzimidazole-based rhodamines 1 and 2 selectively recognize Al 3+ ion in aqueous CH 3 CN (CH 3 CN/H 2 O 4/1 v/v, 10 mM tris HCl buffer, pH 7.0) over the other cations by exhibiting color and "turn-on" emission changes. In contrast, glycine-derived benzimidazole 3 remains silent in the recognition event and emphasizes the role of α-substitution of amino acid undertaken in the design. The fact has been addressed on the basis of the single-crystal X-ray structures and theoretical calculations. Moreover, pink 1·Al 3+ and 2·Al 3+ ensembles selectively sensed F - ions over other halides through a discharge of color. Importantly, compounds 1 and 2 are cell permeable and have been used as imaging reagents for the detection of Al 3+ uptake in human lung carcinoma cell line A549.

Coordination compounds of metals with imidazoles and benzimidazoles

International Nuclear Information System (INIS)

Novikova, G.A.; Molodkin, A.K.; Kukalenko, S.S.

1988-01-01

Methods of preparation, composition and structure of UO 2 2+ , Th 4+ , Mo 3+ , Cd 2+ , Ln 3+ metal ion complexes with imidazoles and benzimidazoles are considered in reviews of native and foreign literature of up to 1985. Complexes are customarily prepared by direct interaction of ligands with inorganic salts in different organic solvents. Complex composition is defined by the nature of complexing metal and inorganic salt anion, ligand volume and basicity, as well as solvent characteristics. Effect of R substituent in imidazole and benzimidazole side chain on composition of coordination compounds is considered

Synthesis, electronic properties, antioxidant and antibacterial activity of some new benzimidazoles.

Science.gov (United States)

Mavrova, Anelia Ts; Yancheva, Denitsa; Anastassova, Neda; Anichina, Kamelya; Zvezdanovic, Jelena; Djordjevic, Aleksandra; Markovic, Dejan; Smelcerovic, Andrija

2015-10-01

Two groups of benzimidazole derivatives were synthesized using as precursors 5(6)-substituted 2-mercapto-benzimidazol-thiols and their antioxidant activity was investigated using TBA-MDA test. In the group of 1,3-disubstituted-benzimidazol-2-imines the highest lipid peroxidation inhibition effect 74.04% (IC₅₀=141.89 μg/mL) revealed ethyl [3-(2-ethoxy-2-oxoethyl)-2-imino-5-benzoyl-2,3-dihydro-1H-benzimdazol-1-yl]acetate 12 while in the group of 2-substituted-1,3-thiazolo[3,2-a]benzimidazolones the highest inhibition effect showed 2-(4-fluorobenzylidene)-7-(phenylcarbonyl)[1,3]thiazolo[3,2-a]benzimidazol-3(2H)-one 17 90.76% (IC₅₀=53.70 μg/mL). In order to estimate the capability of the studied benzimidazoles to act as radical scavengers the structure of the most active derivative within the both subseries was optimized at B3LYP/6-311++G(∗∗) level and the respective bond dissociation enthalpies were calculated. The appropriate models for the HAT and SET-mechanism of the antioxidant activity were proposed. The antibacterial activity of the compounds was evaluated against two Gram-positive bacteria (Bacillus subtilis ATCC 6633 and Staphylococcus aureus ATCC 6538) and three Gram-negative bacteria (Escherichia coli ATCC 8739, Pseudomonas aeruginosa ATCC 9027 and Salmonella abony NCTC 6017). 1,3-Diphenylpropyl-5-methyl-1,3-dihydro-2H-benzimidazol-2-imine 14 exhibited significant activity against B. subtilis, S. aureus, S. abony and E. coli (with MIC values of 0.125, 0.016, 0.50 and 0.50mg/mL, respectively). The group of thiazolobenzimidazolones did not reveal antibacterial activity against the tested strains. Copyright © 2015. Published by Elsevier Ltd.

(Salicylato[tris(1-methyl-1H-benzimidazol-2-ylmethylamine]copper(II perchlorate dimethylformamide disolvate

Directory of Open Access Journals (Sweden)

Huilu Wu

2008-01-01

Full Text Available In the title complex, [Cu(C7H5O3(C27H27N7]ClO4·2C3H7NO, the CuII ion is five-coordinated by four N atoms from the tris(1-methyl-1H-benzimidazol-2-ylmethylamine ligand and an O atom of the monodentate salicylate ligand. The N4O donor set defines a coordination geometry intermediate between square-pyramidal and trigonal–bipyramidal. The crystal structure is stabilized by O—H...O interactions. The atoms of the aromatic ring of the salicylate ligand are disordered over two sites of equal occupancy. In addition, one of the dimethylformamide solvent molecules is partially disordered over two positions, of approximately equal occupancy.

Development and Synthesis of DNA-Encoded Benzimidazole Library.

Science.gov (United States)

Ding, Yun; Chai, Jing; Centrella, Paolo A; Gondo, Chenaimwoyo; DeLorey, Jennifer L; Clark, Matthew A

2018-04-25

Encoded library technology (ELT) is an effective approach to the discovery of novel small-molecule ligands for biological targets. A key factor for the success of the technology is the chemical diversity of the libraries. Here we report the development of DNA-conjugated benzimidazoles. Using 4-fluoro-3-nitrobenzoic acid as a key synthon, we synthesized a 320 million-member DNA-encoded benzimidazole library using Fmoc-protected amino acids, amines and aldehydes as diversity elements. Affinity selection of the library led to the discovery of a novel, potent and specific antagonist of the NK3 receptor.

Boric Acid Catalyzed Convenient Synthesis of Benzimidazoles in Aqueous Media

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Mohammad Reza Poor Heravi

2013-01-01

Full Text Available Synthesis of benzimidazoles has been developed by the o-phenylenediamine with aldehydes using boric acid an efficient catalyst under mild reaction conditions in aqueous media. The product is applicable to aryl and heteroaryl aldehydes. This reaction led to the formation of benzimidazoles new derivatives in good yields. The FT-IR, 19F-NMR, 1H-NMR, 13C-NMR spectra and elemental analysis confirm the structure of compounds.

Boric Acid Catalyzed Convenient Synthesis of Benzimidazoles in Aqueous Media

OpenAIRE

Poor Heravi, Mohammad Reza; Ashori, Marjan

2013-01-01

Synthesis of benzimidazoles has been developed by the o-phenylenediamine with aldehydes using boric acid an efficient catalyst under mild reaction conditions in aqueous media. The product is applicable to aryl and heteroaryl aldehydes. This reaction led to the formation of benzimidazoles new derivatives in good yields. The FT-IR, 19F-NMR, 1H-NMR, 13C-NMR spectra and elemental analysis confirm the structure of compounds.

Fluorescence tuning of 2-(1H-Benzimidazol-2-yl)phenol-ESIPT process

International Nuclear Information System (INIS)

Prakash, S.M.; Jayamoorthy, K.; Srinivasan, N.; Dhanalekshmi, K.I.

2016-01-01

Catalytic synthesis of potential chemosensor 2-(1H-Benzimidazol-2-yl)phenol (HBYP) has been prepared by three components cyclization reaction. It can behaves as a selective fluorescent sensor for the detection of Fe 3+ metal ion. HBYP has been characterized by 1 H NMR, 13 C NMR, mass spectral studies and elemental analysis. Single crystal XRD analysis has been carried out to confirm the structure of HBYP and it shows the imidazole ring is essentially planar and monoclinic crystal. Addition and increasing concentration of Fe 3+ ions into HBYP results dramatic fluorescence quenching. Other cations, including Ca 2+ , Co 2+ , Ni 2+ , Cd 2+ , Pb 2+ , Zn 2+ and Mg 2+ had little influence in the fluorescence intensity. Surprisingly reversible fluorescence enhancement has been observed with the addition of H 3 PO 4 due to the deactivation of iron complex.

New Main Ring control system

International Nuclear Information System (INIS)

Seino, K.; Anderson, L.; Ducar, R.; Franck, A.; Gomilar, J.; Hendricks, B.; Smedinghoff, J.

1990-03-01

The Fermilab Main Ring control system has been operational for over sixteen years. Aging and obsolescence of the equipment make the maintenance difficult. Since the advent of the Tevatron, considerable upgrades have been made to the controls of all the Fermilab accelerators except the Main Ring. Modernization of the equipment and standardization of the hardware and software have thus become inevitable. The Tevatron CAMAC serial system has been chosen as a basic foundation in order to make the Main Ring control system compatible with the rest of the accelerator complex. New hardware pieces including intelligent CAMAC modules have been designed to satisfy unique requirements. Fiber optic cable and repeaters have been installed in order to accommodate new channel requirements onto the already saturated communication medium system. 8 refs., 2 figs

Lectures on algebraic system theory: Linear systems over rings

Science.gov (United States)

Kamen, E. W.

1978-01-01

The presentation centers on four classes of systems that can be treated as linear systems over a ring. These are: (1) discrete-time systems over a ring of scalars such as the integers; (2) continuous-time systems containing time delays; (3) large-scale discrete-time systems; and (4) time-varying discrete-time systems.

Synthesis and biological evaluation of 2-substituted benzimidazole derivatives

Directory of Open Access Journals (Sweden)

Gurusamy Mariappan

2015-09-01

Full Text Available A novel series of 2-substituted benzimidazole derivatives (3a–3j were synthesized by the reaction of 2-chloro methyl benzimidazole with substituted primary aromatic amines. All the compounds were characterized by UV, IR, 1H NMR, mass spectral data and CHN elemental analysis. The synthesized derivatives were screened for analgesic and anti-inflammatory activities. All the compounds showed significant effect at 100 mg/kg p.o. and the experimental data are statistically significant at p < 0.01 level.

Evaluation of chromatographic columns packed with semi- and fully porous particles for benzimidazoles separation.

Science.gov (United States)

Gonzalo-Lumbreras, Raquel; Sanz-Landaluze, Jon; Cámara, Carmen

2015-07-01

The behavior of 15 benzimidazoles, including their main metabolites, using several C18 columns with standard or narrow-bore diameters and different particle size and type were evaluated. These commercial columns were selected because their differences could affect separation of benzimidazoles, and so they can be used as alternative columns. A simple screening method for the analysis of benzimidazole residues and their main metabolites was developed. First, the separation of benzimidazoles was optimized using a Kinetex C18 column; later, analytical performances of other columns using the above optimized conditions were compared and then individually re-optimized. Critical pairs resolution, analysis run time, column type and characteristics, and selectivity were considered for chromatographic columns comparison. Kinetex XB was selected because it provides the shortest analysis time and the best resolution of critical pairs. Using this column, the separation conditions were re-optimized using a factorial design. Separations obtained with the different columns tested can be applied to the analysis of specific benzimidazoles residues or other applications. © 2015 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

Benzimidazole-Based Antibacterial Agents Against F. tularensis

Science.gov (United States)

Kumar, Kunal; Awasthi, Divya; Lee, Seung-Yub; Cummings, Jason E.; Knudson, Susan E.; Slayden, Richard A.; Ojima, Iwao

2013-01-01

Francisella tularensis is a highly virulent pathogenic bacterium. In order to identify novel potential antibacterial agents against F. tularensis, libraries of trisubstituted benzimidazoles were screened against F. tularensis LVS strain. In a preliminary screening assay, remarkably, 23 of 2,5,6- and 2,5,7-trisubstituted benzimidazoles showed excellent activity exhibiting greater than 90 % growth inhibition at 1 µg/mL. Among those hits, 21 compounds showed MIC90 values in the range of 0.35–48.6 µg/mL after accurate MIC determination. In ex-vivo efficacy assays, four of these compounds exhibited 2–3 Log reduction in colony forming units (CFU) per mL at concentrations of 10 and 50 µg/mL. PMID:23623254

Benzimidazole grafted polybenzimidazoles for proton exchange membrane fuel cells

DEFF Research Database (Denmark)

Yang, Jingshuai; Aili, David; Li, Qingfeng

2013-01-01

High molecular weight polybenzimidazole (PBI) was synthesized and grafted with benzimidazole pendant groups. The high molecular weight of PBI resulted in good film-forming properties and superior tensile strength. With a phosphoric acid doping level (ADL) of 13.1, a tensile strength of 16 MPa...... was achieved at room temperature. Grafting of benzimidazole moieties onto the PBI macromolecular chain introduced additional basic sites which allowed the membrane to achieve higher phosphoric acid uptakes. A molar acid conductivity, defined as the specific conductivity of each mole of doping acid...

Facile Synthesis of N -Substituted Benzimidazoles

NARCIS (Netherlands)

Kurhade, Santosh; Rossetti, Arianna; Dömling, Alexander

2016-01-01

A particularly mild and efficient one-pot synthesis of N-substituted benzimidazole derivatives was developed. 2-Fluoro-5-nitrophenylisocyanide reacts with a diverse set of primary amines to afford the respective products in moderate to very good yield (35-95%; 20 examples).

Bis[2-(2-aminoethyl-1H-benzimidazole-κ2N2,N3](nitrato-κ2O,O′cobalt(II chloride trihydrate

Directory of Open Access Journals (Sweden)

Jing Zhao

2012-06-01

Full Text Available In the title compound, [Co(NO3(C9H11N32]Cl·3H2O, the CoII atom is coordinated by four N atoms from two chelating 2-(2-aminoethyl-1H-benzimidazole ligands and two O atoms from one nitrate anion in a distorted octahedral coordination environment. In the crystal, N—H...Cl, N—H...O, O—H...Cl and O—H...O hydrogen bonds link the complex cations, chloride anions and solvent water molecules into a three-dimensional network. π–π interactions between the imidazole and benzene rings and between the benzene rings are observed [centroid–centroid distances = 3.903 (3, 3.720 (3, 3.774 (3 and 3.926 (3 Å].

In vitro susceptibilities of the AIDS-associated microsporidian Encephalitozoon intestinalis to albendazole, its sulfoxide metabolite, and 12 additional benzimidazole derivatives.

OpenAIRE

Katiyar, S K; Edlind, T D

1997-01-01

Recent reports have described the successful treatment of Encephalitozoon intestinalis infection in AIDS patients with albendazole. However, this compound is rapidly metabolized in vivo to albendazole sulfoxide, and furthermore it is only 1 of about 15 commercially developed benzimidazole derivatives. To compare the activities of albendazole, albendazole sulfoxide, and other benzimidazoles, an in vitro system involving infection of green monkey kidney cell (E6) monolayers with E. intestinalis...

Molecular characterization, fitness and mycotoxin production of benzimidazole-resistant isolates of Penicillium expansum.

Science.gov (United States)

Malandrakis, Anastasios A; Markoglou, Anastasios N; Konstantinou, Sotiris; Doukas, Eleftherios G; Kalampokis, John F; Karaoglanidis, George S

2013-04-01

Penicillium expansum field-strains resistant to benzimidazole fungicides were isolated in high frequency from decayed apple fruit collected from packinghouses and processing industries located in the region of Imathia, N. Greece. In vitro fungitoxicity tests resulted in the identification of two different resistant phenotypes: highly (BEN-HR) and moderately (BEN-MR) carbendazim-resistant. Thirty seven percent of the isolated P. expansum strains belonged to the BEN-HR phenotype, carried no apparent fitness penalties and exhibited resistance levels higher than 60 based on EC50 values. Cross resistance studies with other benzimidazole fungicides showed that all BEN-HR and BEN-MR isolates were also less sensitive to benomyl and thiabendazole. Fungitoxicity tests on the response of BEN-HR isolates to fungicides belonging to other chemical classes revealed no cross-resistance relationships between benzimidazoles and the phenylpyrrole fludioxonil, the dicarboximide iprodione, the anilinopyrimidine cyprodinil, the QoI pyraclostrobin, the imidazole imazalil and the triazole tebuconazole, indicating that a target-site modification is probably responsible for the BEN-HR phenotype observed. Contrary to the above, some BEN-MR isolates exhibited an increased sensitivity to cyprodinil compared to benzimidazole-sensitive ones. BEN-MR isolates had fitness parameters similar to the benzimidazole-sensitive isolates except for conidia production which appeared significantly decreased. Analysis of mycotoxin production (patulin and citrinin) showed that all benzimidazole-resistant isolates produced mycotoxins at concentrations significantly higher than sensitive isolates both on culture medium and on artificially inoculated apple fruit. Comparison of the β-tubulin gene DNA sequence between resistant and sensitive isolates revealed a point mutation resulting from the E198A substitution of the corresponding protein in most but not all HR isolates tested. Molecular analysis of the �

Virtual Exploration of the Ring Systems Chemical Universe.

Science.gov (United States)

Visini, Ricardo; Arús-Pous, Josep; Awale, Mahendra; Reymond, Jean-Louis

2017-11-27

Here, we explore the chemical space of all virtually possible organic molecules focusing on ring systems, which represent the cyclic cores of organic molecules obtained by removing all acyclic bonds and converting all remaining atoms to carbon. This approach circumvents the combinatorial explosion encountered when enumerating the molecules themselves. We report the chemical universe database GDB4c containing 916 130 ring systems up to four saturated or aromatic rings and maximum ring size of 14 atoms and GDB4c3D containing the corresponding 6 555 929 stereoisomers. Almost all (98.6%) of these ring systems are unknown and represent chiral 3D-shaped macrocycles containing small rings and quaternary centers reminiscent of polycyclic natural products. We envision that GDB4c can serve to select new ring systems from which to design analogs of such natural products. The database is available for download at www.gdb.unibe.ch together with interactive visualization and search tools as a resource for molecular design.

Diversity-Oriented Synthesis of Coumarin-Linked Benzimidazoles via a One-Pot, Three-Step, Intramolecular Knoevenagel Cyclization.

Science.gov (United States)

Yao, Po-Hsin Eric; Kumar, Sunil; Liu, Yu-Li; Fang, Chiu-Ping; Liu, Chia-Chen; Sun, Chung-Ming

2017-04-10

Diversity-oriented synthesis of coumarin-linked benzimidazoles from N-(2-aminophenyl)-2-cyanoacetamide was achieved via a one-pot, three-step sequential reaction in excellent yields. In situ intramolecular cyclization of the cyanoacetamide afforded benzimidazoles which subsequently underwent a Knoevenagel condensation of the 2-cyanomethylbenzimidazoles with salicylaldehydes promoted by triethylamine to reach the target compounds. An important intermediate, 2-(2-imino-2H-chromen-3-yl)-1H-benzimidazole was characterized by X-ray analysis and further hydrolyzed to 2-(coumarin-3-yl)benzimidazole in acidic condition. Among the synthesized compounds, some were found to be promising inhibitors of porcine kidney d-amino acid oxidase (pkDAO).

Antihelminthic benzimidazoles are novel HIF activators that prevent oxidative neuronal death via binding to tubulin.

Science.gov (United States)

Aleyasin, Hossein; Karuppagounder, Saravanan S; Kumar, Amit; Sleiman, Sama; Basso, Manuela; Ma, Thong; Siddiq, Ambreena; Chinta, Shankar J; Brochier, Camille; Langley, Brett; Haskew-Layton, Renee; Bane, Susan L; Riggins, Gregory J; Gazaryan, Irina; Starkov, Anatoly A; Andersen, Julie K; Ratan, Rajiv R

2015-01-10

Pharmacological activation of the adaptive response to hypoxia is a therapeutic strategy of growing interest for neurological conditions, including stroke, Huntington's disease, and Parkinson's disease. We screened a drug library with known safety in humans using a hippocampal neuroblast line expressing a reporter of hypoxia-inducible factor (HIF)-dependent transcription. Our screen identified more than 40 compounds with the ability to induce hypoxia response element-driven luciferase activity as well or better than deferoxamine, a canonical activator of hypoxic adaptation. Among the chemical entities identified, the antihelminthic benzimidazoles represented one pharmacophore that appeared multiple times in our screen. Secondary assays confirmed that antihelminthics stabilized the transcriptional activator HIF-1α and induced expression of a known HIF target gene, p21(cip1/waf1), in post-mitotic cortical neurons. The on-target effect of these agents in stimulating hypoxic signaling was binding to free tubulin. Moreover, antihelminthic benzimidazoles also abrogated oxidative stress-induced death in vitro, and this on-target effect also involves binding to free tubulin. These studies demonstrate that tubulin-binding drugs can activate a component of the hypoxic adaptive response, specifically the stabilization of HIF-1α and its downstream targets. Tubulin-binding drugs, including antihelminthic benzimidazoles, also abrogate oxidative neuronal death in primary neurons. Given their safety in humans and known ability to penetrate into the central nervous system, antihelminthic benzimidazoles may be considered viable candidates for treating diseases associated with oxidative neuronal death, including stroke.

Synthesis, crystal structure determination and antiproliferative activity of novel 2-amino-4-aryl-4,10-dihydro[1,3,5]triazino[1,2- a]benzimidazoles

Science.gov (United States)

Hranjec, Marijana; Pavlović, Gordana; Karminski-Zamola, Grace

2012-01-01

This manuscript describes the synthesis of novel 2-amino-4-aryl-4,10-dihydro-[1,3,5]triazino[1,2- a]benzimidazoles as hydrochloride salts 4a-n and 5b which were prepared in the reaction of cyclocondensation between 2-guanidinobenzimidazole and versatile heteroaromatic aldehydes. Structures of all prepared compounds have been studied by using 1H and 13C NMR, IR and UV/Vis spectroscopy. The crystal and molecular structure of 4f was determined by X-ray diffraction on single crystals. The molecule of 2-amino-4-(4'-methylphenyl)-4,10-dihydro[1,3,5]triazino[1,2- a]benzimidazole hydrochloride 4f (C 16H 16N 5+·Cl -) exists in the solid state in one of the possible tautomeric forms, being protonated at the one of the nitrogen atoms of the 1,4-dihydrotriazine ring. The molecule is highly delocalized within the 4,10-dihydro[1,3,5]triazino[1,2- a]benzimidazole moiety with the highest deviation from the plane for the methine carbon atom and the protonated nitrogen atom of the 1,4-dihydrotriazine ring. The cations are joined via N-H⋯N hydrogen bonds into R22(8) centrosymmetric dimers. Cation dimers are further connected with Cl - ions via N-H⋯Cl and C-H⋯Cl hydrogen bonds into 2D chains spreading along the b axis. The obtained single-crystal X-ray structure determination unequivocally confirms tautomeric form of the compound present in the solid-state and can represent tantative pattern for other prepared compounds. All prepared compounds were tested on their antiproliferative activity in vitro on several human cancer cell lines. Compound 4m was the most active one (IC 50 ≈ 20 μM), while compounds 4d, 4f, 4k, 4l4m showed moderate, but non-selective, antiproliferative activity with IC 50 25-60 μM.

The Synthesis of Dicationic Extended Bis-Benzimidazoles

OpenAIRE

Kang, Zhijan; Dykstra, Christine C.; Boykin, David W.

2004-01-01

The synthesis of extended dicationic bis-benzimidazoles starting from trans-1,2-bis(4-cyanophenyl)ethene and trans-1,2-bis(4-cyanophenyl)cyclopropane is reported. The target diamidines show significant in vitro activity against B. subtilis.

Lead optimization of 2-(piperidin-3-yl)-1H-benzimidazoles: identification of 2-morpholin- and 2-thiomorpholin-2-yl-1H-benzimidazoles as selective and CNS penetrating H₁-antihistamines for insomnia.

Science.gov (United States)

Ravula, Satheesh Babu; Yu, Jinghua; Tran, Joe A; Arellano, Melissa; Tucci, Fabio C; Moree, Wilna J; Li, Bin-Feng; Petroski, Robert E; Wen, Jianyun; Malany, Siobhan; Hoare, Samuel R J; Madan, Ajay; Crowe, Paul D; Beaton, Graham

2012-01-01

The structure-activity relationships of 2-(piperidin-3-yl)-1H-benzimidazoles, 2-morpholine and 2-thiomorpholin-2-yl-1H-benzimidazoles are described. In the lead optimization process, the pK(a) and/or logP of benzimidazole analogs were reduced either by attachment of polar substituents to the piperidine nitrogen or incorporation of heteroatoms into the piperidine heterocycle. Compounds 9a and 9b in the morpholine series and 10g in the thiomorpholine series demonstrated improved selectivity and CNS profiles compared to lead compound 2 and these are potential candidates for evaluation as sedative hypnotics. Copyright © 2011 Elsevier Ltd. All rights reserved.

Benzimidazole for the prevention of toxic effects of air pollutants on plants

Energy Technology Data Exchange (ETDEWEB)

Takaoka, I; Fukuda, M; Kitano, H; Shinohara, T

1974-02-02

Tobacco plants were sprayed with benzimidazole before being exposed to 30 ppM of photochemical oxidants for a period of two hours. The plants were observed 48 hours after exposure and found to have suffered no toxic effects from the oxidants. It may be concluded that benzimidazole is an effective agent for preventing the toxic effects of air pollutants, such as photochemical oxidants on plants.

Imidazoles and benzimidazoles as tubulin-modulators for anti-cancer therapy.

Science.gov (United States)

Torres, Fernando C; García-Rubiño, M Eugenia; Lozano-López, César; Kawano, Daniel F; Eifler-Lima, Vera L; von Poser, Gilsane L; Campos, Joaquín M

2015-01-01

Imidazoles and benzimidazoles are privileged heterocyclic bioactive compounds used with success in the clinical practice of innumerous diseases. Although there are many advancements in cancer therapy, microtubules remain as one of the few macromolecular targets validated for planning active anti-cancer compounds, and the design of drugs that modulate microtubule dynamics in unknown sites of tubulin is one of the goals of the medicinal chemistry. The discussion of the role of new and commercially available imidazole and benzimidazole derivatives as tubulin modulators is scattered throughout scientific literature, and indicates that these compounds have a tubulin modulation mechanism different from that of tubulin modulators clinically available, such as paclitaxel, docetaxel, vincristine and vinblastine. In fact, recent literature indicates that these derivatives inhibit microtubule formation binding to the colchicine site, present good pharmacokinetic properties and are capable of overcoming multidrug resistance in many cell lines. The understanding of the mechanisms involved in the imidazoles/benzimidazoles modulation of microtubule dynamics is very important to develop new strategies to overcome the resistance to anti-cancer drugs and to discover new biomarkers and targets for cancer chemotherapy.

The inhibition performance of long-chain alkyl-substituted benzimidazole derivatives for corrosion of mild steel in HCl

International Nuclear Information System (INIS)

Zhang, Dongqin; Tang, Yongming; Qi, Sijun; Dong, Dawei; Cang, Hui; Lu, Gang

2016-01-01

Highlights: • Inhibition performance of long-chain alkyl-substituted benzimidazole. • Benzimidazole segment donating electrons to metal surface. • Non-polar long chain enhancing inhibition by the barrier effect. • Molecular form of DBI more tightly adsorbs on the steel than its protonated form. - Abstract: The corrosion inhibition of a new benzimidazole derivative, 6-(dodecyloxy)-1H-benzo[d]imidazole (DBI), for mild steel in 1 M HCl was investigated in this paper. Computational chemistry was performed to explore the adsorption of DBI on metal surface. Inhibition performance of DBI is attributed to both the direct interaction of benzimidazole segment with iron surface and the barrier effect of the non-polar long chain against aggressive solution. Compared to the protonated form, the molecular form of DBI could more tightly interact with iron surface. These results show that the long-chain alkyl-substituted benzimidazole derivative is of great potential application as corrosion inhibitor.

Microwave-assisted synthesis of some nitro-benzimidazoles and their salicyl and isatin Schiff bases

Directory of Open Access Journals (Sweden)

F. Yılmaz

2017-11-01

Full Text Available A series of 5-nitrosubstituted benzimidazole and 6-nitro substituted benzimidazole derivatives were synthesized starting from iminoester hydrochloride and 4-nitro-o-phenylenediamine under microwave irradiation. The structure of newly synthesized compounds was confirmed by IR, 1H-NMR, 13C-NMR, LC-MS spectroscopy and elemental analysis.

Antimalarial pyrido[1,2-a]benzimidazoles.

Science.gov (United States)

Ndakala, Albert J; Gessner, Richard K; Gitari, Patricia W; October, Natasha; White, Karen L; Hudson, Alan; Fakorede, Foluke; Shackleford, David M; Kaiser, Marcel; Yeates, Clive; Charman, Susan A; Chibale, Kelly

2011-07-14

A novel class of antimalarial pyrido[1,2-a]benzimidazoles were synthesized and evaluated for antiplasmodial activity and cytotoxicity following hits identified from screening commercially available compound collections. The most active of these, TDR86919 (4c), showed improved in vitro activity vs the drug-resistant K1 strain of Plasmodium falciparum relative to chloroquine (IC(50) = 0.047 μM v 0.17 μM); potency was retained against a range of drug-sensitive and drug-resistant strains, with negligible cytotoxicity against the mammalian (L-6) cell line (selectivity index of >600). 4c and several close analogues (as HCl or mesylate salts) showed significant efficacy in P. berghei infected mice following both intraperitoneal (ip) and oral (po) administration, with >90% inhibition of parasitemia, accompanied by an increase in the mean survival time (MSD). The pyrido[1,2-a]benzimidazoles appeared to be relatively slow acting in vivo compared to chloroquine, and metabolic stability of the alkylamino side chain was identified as a key issue in influencing in vivo activity.

Effect of substituents on polarizability and hyperpolarizability values of benzimidazole metal complexes

Energy Technology Data Exchange (ETDEWEB)

Praveen, P. A.; Babu, R. Ramesh, E-mail: rampap2k@yahoo.co.in [Crystal Growth and Thin films Laboratory, Department of Physics, Bharathidasan University, Tiruchirappalli - 620 024, Tamilnadu (India)

2016-05-23

In this report, the polarizability and first and second order hyperpolarizability values of bis benzimidazole Zn(II)-2R and bis benzimidazole Cd(II)-2R complexes, with different electron donating moieties R (R= Cl, Br, I, Acetate) were calculated using time dependent Hartree-Fock (TDHF) formalism embedded in MOPAC2012 package. Further the role of substituents on polarizability and hyperpolarizability values is investigated for the first time by analyzing the frontier molecular orbitals of the complexes with respect to the electronegativity of the substituents. It is found that the increase in electronegativity of the substituents correspondingly increases the energy gap of the molecules, which in turn reduces the polarizability values of both Zn and Cd benzimidazole complexes. Similarly, increase in electronegativity reduces the electric quadrupole moments of both the metal complexes, which in turn reduces the hyperpolarizability values.

Triphenylamine based benzimidazole and benzothiazole: Synthesis and applications in fluorescent chemosensors and laser dyes

Energy Technology Data Exchange (ETDEWEB)

Yang, Yang [State Key Laboratory of Luminescence and Applications, Changchun Institute of Optics Fine Mechanics and Physics, Chinese Academy of Sciences, Changchun 130033 (China); University of Chinese Academy of Sciences, Beijing 100039 (China); Li, Bin, E-mail: libinteacher@163.com [State Key Laboratory of Luminescence and Applications, Changchun Institute of Optics Fine Mechanics and Physics, Chinese Academy of Sciences, Changchun 130033 (China); Zhang, Liming; Guan, Yunlong [State Key Laboratory of Luminescence and Applications, Changchun Institute of Optics Fine Mechanics and Physics, Chinese Academy of Sciences, Changchun 130033 (China)

2014-01-15

Triphenylamine based fluorescent dyes TPA-benzimidazole and TPA-benzothiazole have been designed and synthesized. The TPA-benzimidazole chemosensor was tested for a number of metal ions and found to exhibit binding affinity for Fe{sup 3+} and Hg{sup 2+} in acetonitrile, and the fluorescence quenching was achieved through a PET process. The appearance of an isosbestic point in absorption titrations and Job's plot analysis supported 1:1 stoichiometries for Fe{sup 3+} and Hg{sup 2+} ions. Laser experiments showed that under transversal pumping with a Q-switched Nd:YAG (355 nm) laser in toluene, TPA-benzothiazole exhibits efficient and stable amplified spontaneous emissions (ASE) at 436 nm. -- Highlights: • Triphenylamine based fluorescent dyes TPA-benzimidazole and TPA-benzothiazole have been designed and synthesized. • The TPA-benzimidazole exhibits binding affinity for Fe{sup 3+} and Hg{sup 2+} in acetonitrile and the fluorescence quenching was achieved through a PET process. • Under transversal pumping at 355 nm in toluene, TPA-benzothiazole exhibits efficient and stable amplified spontaneous emissions (ASE) in 436 nm.

Triphenylamine based benzimidazole and benzothiazole: Synthesis and applications in fluorescent chemosensors and laser dyes

International Nuclear Information System (INIS)

Yang, Yang; Li, Bin; Zhang, Liming; Guan, Yunlong

2014-01-01

Triphenylamine based fluorescent dyes TPA-benzimidazole and TPA-benzothiazole have been designed and synthesized. The TPA-benzimidazole chemosensor was tested for a number of metal ions and found to exhibit binding affinity for Fe 3+ and Hg 2+ in acetonitrile, and the fluorescence quenching was achieved through a PET process. The appearance of an isosbestic point in absorption titrations and Job's plot analysis supported 1:1 stoichiometries for Fe 3+ and Hg 2+ ions. Laser experiments showed that under transversal pumping with a Q-switched Nd:YAG (355 nm) laser in toluene, TPA-benzothiazole exhibits efficient and stable amplified spontaneous emissions (ASE) at 436 nm. -- Highlights: • Triphenylamine based fluorescent dyes TPA-benzimidazole and TPA-benzothiazole have been designed and synthesized. • The TPA-benzimidazole exhibits binding affinity for Fe 3+ and Hg 2+ in acetonitrile and the fluorescence quenching was achieved through a PET process. • Under transversal pumping at 355 nm in toluene, TPA-benzothiazole exhibits efficient and stable amplified spontaneous emissions (ASE) in 436 nm

Fluorescent silica hybrid materials containing benzimidazole dyes obtained by sol-gel method and high pressure processing

International Nuclear Information System (INIS)

Hoffmann, Helena Sofia; Stefani, Valter; Benvenutti, Edilson Valmir; Costa, Tania Maria Haas; Gallas, Marcia Russman

2011-01-01

Research highlights: → Sol-gel technique was used to obtain silica based hybrid materials containing benzimidazole dyes. → The sol-gel catalysts, HF and NaF, produce xerogels with different optical and textural characteristics. → High pressure technique (6.0 GPa) was used to produce fluorescent and transparent silica compacts with the dyes entrapped in closed pores, maintaining their optical properties. → The excited state intramolecular proton transfer (ESIPT) mechanism of benzimidazole dyes was studied by steady-state fluorescence spectroscopy for the monoliths, powders, and compacts. - Abstract: New silica hybrid materials were obtained by incorporation of two benzimidazole dyes in the silica network by sol-gel technique, using tetraethylorthosilicate (TEOS) as inorganic precursor. Several syntheses were performed with two catalysts (HF and NaF) producing powders and monoliths with different characteristics. The dye 2-(2'-hydroxy-5'-aminophenyl)benzimidazole was dispersed and physically adsorbed in the matrix, and the dye 2'(5'-N-(3-triethoxysilyl)propylurea-2'-hydroxyphenyl)benzimidazole was silylated, becoming chemically bonded to the silica network. High pressure technique was used to produce fluorescent and transparent silica compacts with the silylated and incorporated dye, at 6.0 GPa and room temperature. The excited state intramolecular proton transfer (ESIPT) mechanism of benzimidazole dyes was studied by steady-state fluorescence spectroscopy for the monoliths, powders, and compacts. The influence of the syntheses conditions was investigated by textural analysis using nitrogen adsorption isotherms.

Microwave promoted simple, efficient and regioselective synthesis of trisubstituted imidazo[1,2-a]benzimidazoles on soluble support.

Science.gov (United States)

Chen, Li-Hsun; Hsiao, Ya-Shan; Yellol, Gorakh S; Sun, Chung-Ming

2011-03-14

An efficient microwave-assisted and soluble polymer-supported synthesis of medicinally important imidazole-fused benzimidazoles has been developed. The protocol involves the rapid condensation of polymer-bound amino benzimidazoles with various α-bromoketones and subsequent in situ intramolecular cyclization under microwave irradiation resulting in a one pot synthesis of imidazole interlacing benzimidazole polymer conjugates. The condensed product was obtained with excellent regioselectivity. The biologically interesting imidazo[1,2-a]benzimidazoles was released from polymer support at ambient temperature. Diversity in the triheterocyclic nucleus was achieved by the different substitutions at its 2, 3, and 9 positions. The new protocol has the advantages of short reaction time, easy workup process, excellent yields, reduced environmental impact, wide substrate scope and convenient procedure.

Interaction of Benzimidazoles and Benzotriazole: Its Corrosion Protection Properties on Mild Steel in Hydrochloric Acid

Science.gov (United States)

Ramya, K.; Mohan, Revathi; Joseph, Abraham

2014-11-01

Synergistic hydrogen-bonded interaction of alkyl benzimidazoles and 1,2,3-benzotrizole and its corrosion protection properties on mild steel in hydrochloric acid at different temperatures have been studied using polarization, EIS, adsorption, surface studies, and computational methods. The extent of synergistic interaction increases with temperature. Quantum chemical approach is used to calculate some electronic properties of the molecules and to ascertain the synergistic interaction, inhibitive effect, and molecular structures. The corrosion inhibition efficiencies and the global chemical reactivity relate to some parameters, such as total energy, E HOMO, E LUMO, and gap energy (Δ E). 1,2,3-Benzotrizole interacts with benzimidazoles derivatives up to a bond length of approximately 1.99 Å. This interaction represents the formation of a hydrogen bond between the 1,2,3-benzotrizole and benzimidazoles. This synergistic interaction of 1,2,3-benzotrizole and benzimidazole derivatives offers extended inhibition efficiency toward mild steel in hydrochloric acid.

Synthesis and properties of mixed-ligand ruthenium(II) complexes containing 2-(2-pyridyl)-benzimidazole and related ligands

International Nuclear Information System (INIS)

Haga, Masaaki; Tanaka, Toshio.

1979-01-01

Mixed-ligand ruthenium(II) complexes of the [Ru(bpy) 2 L]sup(n+) (ClO 4 )sub(n) type, where bpy= 2,2'-bipyridine; L= 2-(2-pyridyl)-benzimidazole (PBImH) when n= 2, and L= 2-(2-pyridyl)-benzimidazolate (PBIm) and 2-(o-hydroxyphenyl)-benzimidazole (OBImH) when n= 1, were prepared. Anodic peak potentials and ruthenium-to-bipyridine charge transfer bands of these complexes are rationalized in terms of the donor ability of L. (author)

Synthesis and properties of mixed-ligand ruthenium(II) complexes containing 2-(2-pyridyl)-benzimidazole and related ligands

Energy Technology Data Exchange (ETDEWEB)

Haga, M [Mie Univ., Tsu (Japan); Tanaka, T

1979-07-01

Mixed-ligand ruthenium(II) complexes of the (Ru(bpy)/sub 2/L)sup(n+) (ClO/sub 4/)sub(n) type, where bpy= 2,2'-bipyridine; L= 2-(2-pyridyl)-benzimidazole (PBImH) when n= 2, and L= 2-(2-pyridyl)-benzimidazolate (PBIm) and 2-(o-hydroxyphenyl)-benzimidazole (OBImH) when n= 1, were prepared. Anodic peak potentials and ruthenium-to-bipyridine charge transfer bands of these complexes are rationalized in terms of the donor ability of L.

Benzimidazoles diminish ERE transcriptional activity and cell growth in breast cancer cells

Energy Technology Data Exchange (ETDEWEB)

Payton-Stewart, Florastina [Department of Chemistry, College of Arts and Sciences, Xavier University of Louisiana, New Orleans, LA (United States); Tilghman, Syreeta L. [Division of Basic Pharmaceutical Sciences, College of Pharmacy, Xavier University of Louisiana, New Orleans, LA (United States); Williams, LaKeisha G. [Division of Clinical and Administrative Sciences, College of Pharmacy Xavier University of Louisiana, New Orleans, LA (United States); Winfield, Leyte L., E-mail: lwinfield@spelman.edu [Department of Chemistry, Spelman College, Atlanta, GA (United States)

2014-08-08

Highlights: • The methyl-substituted benzimidazole was more effective at inhibiting growth in MDA-MB 231 cells. • The naphthyl-substituted benzimidazole was more effective at inhibiting growth in MCF-7 cells than ICI. • The benzimidazole molecules demonstrated a dose-dependent reduction in ERE transcriptional activity. • The benzimidazole molecules had binding mode in ERα and ERβ comparable to that of the co-crystallized ligand. - Abstract: Estrogen receptors (ERα and ERβ) are members of the nuclear receptor superfamily. They regulate the transcription of estrogen-responsive genes and mediate numerous estrogen related diseases (i.e., fertility, osteoporosis, cancer, etc.). As such, ERs are potentially useful targets for developing therapies and diagnostic tools for hormonally responsive human breast cancers. In this work, two benzimidazole-based sulfonamides originally designed to reduce proliferation in prostate cancer, have been evaluated for their ability to modulate growth in estrogen dependent and independent cell lines (MCF-7 and MDA-MB 231) using cell viability assays. The molecules reduced growth in MCF-7 cells, but differed in their impact on the growth of MDA-MB 231 cells. Although both molecules reduced estrogen response element (ERE) transcriptional activity in a dose dependent manner, the contrasting activity in the MDA-MB-231 cells seems to suggest that the molecules may act through alternate ER-mediated pathways. Further, the methyl analog showed modest selectivity for the ERβ receptor in an ER gene expression array panel, while the naphthyl analog did not significantly alter gene expression. The molecules were docked in the ligand binding domains of the ERα-antagonist and ERβ-agonist crystal structures to evaluate the potential of the molecules to interact with the receptors. The computational analysis complimented the results obtained in the assay of transcriptional activity and gene expression suggesting that the molecules

Benzimidazoles diminish ERE transcriptional activity and cell growth in breast cancer cells

International Nuclear Information System (INIS)

Payton-Stewart, Florastina; Tilghman, Syreeta L.; Williams, LaKeisha G.; Winfield, Leyte L.

2014-01-01

Highlights: • The methyl-substituted benzimidazole was more effective at inhibiting growth in MDA-MB 231 cells. • The naphthyl-substituted benzimidazole was more effective at inhibiting growth in MCF-7 cells than ICI. • The benzimidazole molecules demonstrated a dose-dependent reduction in ERE transcriptional activity. • The benzimidazole molecules had binding mode in ERα and ERβ comparable to that of the co-crystallized ligand. - Abstract: Estrogen receptors (ERα and ERβ) are members of the nuclear receptor superfamily. They regulate the transcription of estrogen-responsive genes and mediate numerous estrogen related diseases (i.e., fertility, osteoporosis, cancer, etc.). As such, ERs are potentially useful targets for developing therapies and diagnostic tools for hormonally responsive human breast cancers. In this work, two benzimidazole-based sulfonamides originally designed to reduce proliferation in prostate cancer, have been evaluated for their ability to modulate growth in estrogen dependent and independent cell lines (MCF-7 and MDA-MB 231) using cell viability assays. The molecules reduced growth in MCF-7 cells, but differed in their impact on the growth of MDA-MB 231 cells. Although both molecules reduced estrogen response element (ERE) transcriptional activity in a dose dependent manner, the contrasting activity in the MDA-MB-231 cells seems to suggest that the molecules may act through alternate ER-mediated pathways. Further, the methyl analog showed modest selectivity for the ERβ receptor in an ER gene expression array panel, while the naphthyl analog did not significantly alter gene expression. The molecules were docked in the ligand binding domains of the ERα-antagonist and ERβ-agonist crystal structures to evaluate the potential of the molecules to interact with the receptors. The computational analysis complimented the results obtained in the assay of transcriptional activity and gene expression suggesting that the molecules

APS storage ring vacuum system performance

International Nuclear Information System (INIS)

Noonan, J.R.; Gagliano, J.; Goeppner, G.A.

1997-01-01

The Advanced Photon Source (APS) storage ring was designed to operated with 7-GeV, 100-mA positron beam with lifetimes > 20 hours. The lifetime is limited by residual gas scattering and Touschek scattering at this time. Photon-stimulated desorption and microwave power in the rf cavities are the main gas loads. Comparison of actual system gas loads and design calculations will be given. In addition, several special features of the storage ring vacuum system will be presented

Benzimidazole as corrosion inhibitor for heat treated 6061 Al- SiCp composite in acetic acid

International Nuclear Information System (INIS)

Chacko, Melby; Nayak, Jagannath

2015-01-01

6061 Al-SiCpcomposite was solutionizedat 350 °C for 30 minutes and water quenched. It was then underaged at 140 °C (T6 treatment). The aging behaviour of the composite was studied using Rockwell B hardness measurement. Corrosion behaviour of the underaged sample was studied in different concentrations of acetic acid and at different temperatures. Benzimidazole at different concentrations was used for the inhibition studies. Inhibition efficiency of benzimidazole was calculated for different experimental conditions. Thermodynamic parameters were found out which suggested benzimidazole is an efficient inhibitor and it adsorbed on to the surface of composite by mixed adsorption where chemisorption is predominant. (paper)

Cavity Ring-down Spectroscopic System And Method

KAUST Repository

Alquaity, Awad Bin Saud

2015-05-14

A system and method for cavity ring-down spectroscopy can include a pulsed quantum cascade laser, an optical ring-down cavity, a photodetector, and an oscilloscope. The system and method can produce pulse widths of less than 200 ns with bandwidths greater than 300 pm, as well as provide temporal resolution of greater than 10 .mu.s.

Cavity Ring-down Spectroscopic System And Method

KAUST Repository

Alquaity, Awad Bin Saud; Farooq, Aamir

2015-01-01

A system and method for cavity ring-down spectroscopy can include a pulsed quantum cascade laser, an optical ring-down cavity, a photodetector, and an oscilloscope. The system and method can produce pulse widths of less than 200 ns with bandwidths greater than 300 pm, as well as provide temporal resolution of greater than 10 .mu.s.

Evaluation of the Membrane Permeability (PAMPA and Skin) of Benzimidazoles with Potential Cannabinoid Activity and their Relation with the Biopharmaceutics Classification System (BCS)

OpenAIRE

Alvarez-Figueroa, M. Javiera; Pessoa-Mahana, C. David; Palavecino-González, M. Elisa; Mella-Raipán, Jaime; Espinosa-Bustos, Cristián; Lagos-Muñoz, Manuel E.

2011-01-01

The permeability of five benzimidazole derivates with potential cannabinoid activity was determined in two models of membranes, parallel artificial membrane permeability assay (PAMPA) and skin, in order to study the relationship of the physicochemical properties of the molecules and characteristics of the membranes with the permeability defined by the Biopharmaceutics Classification System. It was established that the PAMPA intestinal absorption method is a good predictor for classifying thes...

Benzimidazoles as benzamide replacements within cyclohexane-based CC chemokine receptor 2 (CCR2) antagonists.

Science.gov (United States)

Cherney, Robert J; Mo, Ruowei; Meyer, Dayton T; Pechulis, Anthony D; Guaciaro, Michael A; Lo, Yvonne C; Yang, Gengjie; Miller, Persymphonie B; Scherle, Peggy A; Zhao, Qihong; Cvijic, Mary Ellen; Barrish, Joel C; Decicco, Carl P; Carter, Percy H

2012-10-01

We describe the design, synthesis, and evaluation of benzimidazoles as benzamide replacements within a series of trisubstituted cyclohexane CCR2 antagonists. 7-Trifluoromethylbenzimidazoles displayed potent binding and functional antagonism of CCR2 while being selective over CCR3. These benzimidazoles were also incorporated into lactam-containing antagonists, thus completely eliminating the customary bis-amide. Copyright © 2012 Elsevier Ltd. All rights reserved.

QSAR study of benzimidazole derivatives inhibition on escherichia ...

African Journals Online (AJOL)

The paper describes a quantitative structure-activity relationship (QSAR) study of IC50 values of benzimidazole derivatives on escherichia coli methionine aminopeptidase. The activity of the 32 inhibitors has been estimated by means of multiple linear regression (MLR) and artificial neural network (ANN) techniques.

Anion exchange membrane based on alkali doped poly(2,5-benzimidazole) for alkaline membrane fuel cell

CSIR Research Space (South Africa)

Luo, H

2010-03-01

Full Text Available was prepared. The alkali doped poly(2,5-benzimidazole) membrane is a promising candidate as anion exchange membrane for fuel cell application. The alkali doped poly(2,5-benzimidazole) membrane reached an anion conductivity of 2.3×10-2 S cm-1 at room temperature...

Synthesis of benzimidazoles by potassium tert-butoxide-promoted intermolecular cyclization reaction of 2-iodoanilines with nitriles.

Science.gov (United States)

Xiang, Shi-Kai; Tan, Wen; Zhang, Dong-Xue; Tian, Xian-Li; Feng, Chun; Wang, Bi-Qin; Zhao, Ke-Qing; Hu, Ping; Yang, Hua

2013-11-14

The synthesis of benzimidazoles by intermolecular cyclization reaction of 2-iodoanilines with nitriles has been developed. These reactions proceeded without the aid of any transition metals or ligands and just using KOBu(t) as the base. A variety of substituted benzimidazole derivatives can be synthesized by the approach.

Thermodynamics of the Sorption of Benzimidazoles on Octadecyl Silica Gel from Water-Methanol Eluents

Science.gov (United States)

Shafigulin, R. V.; Bulanova, A. V.

2018-02-01

The standard enthalpy and entropy component of transferring benzimidazoles from water-methanol solutions to surfaces of octadecyl silica gel are determined using reversed-phase high-performance liquid chromatography (RP HPLC). The dependences between the enthalpy and polarizability of the molecules of the studied benzimidazoles, the enthalpy and the entropy factor are studied, and the influence of the quantitative composition of the water-methanol solution on the enthalpy are studied.

The Conversion of Wiswesser Line Notations to Ring Codes. I. The Conversion of Ring Systems

Science.gov (United States)

Granito, Charles E.; And Others

1972-01-01

The computerized conversion of Wiswesser Line Notations to Ring Codes, using a two-part approach, and the set of computer programs generated for the conversion of ring systems are described. (9 references) (Author)

Concurrent coordination of ligand in metal chloride complexes with 1-vinyl-2-(2-pyridyl)benzimidazole

International Nuclear Information System (INIS)

Bajkalov, L.V.; Domnina, E.S.

1996-01-01

The properties and structure of bivalent cadmium and 1-vinyl-2-(2-pyridyl)benzimidazole chloride complexes, which have been prepared for the first time, have been studied by the methods of potentiometric titration and PMR, 35 Cl NQR, UV and IR spectroscopy. For the complexes above di- and polymeric structures in crystal phase are suggested, where ligand plays the role of a bridge. N,N-bidentate ligand. In solution the complexes dissociate with formation of monomeric coordination compounds, their metal being bound by different ways, stemming from participation of N benzimidazole or pyridine fragment of the ligand. Adducts of ionic type with second sphere 1-vinyl-2-(2-pyridyl)benzimidazole cation have been obtained in the course of hydrochlorination of the complexes prepared

2-(1H-Benzimidazol-2-ylphenol

Directory of Open Access Journals (Sweden)

S. M. Prakash

2014-02-01

Full Text Available The title molecule, C13H10N2O, is essentially planar, the maximum deviation from the plane of the non-H atoms being 0.016 (2 Å. The imidazole ring makes a dihedral angle of 0.37 (13° with the attached benzene ring. An intramolecular O—H...N hydrogen bond generates an S(6 ring motif. In the crystal, molecules are linked through N—H...O hydrogen bonds, forming chains propagating in [001]. The crystal packing also features four π–π stacking interactions involving the imidazole ring, fused benzene ring and attached benzene ring system [centroid–centroid distances = 3.6106 (17, 3.6108 (17, 3.6666 (17 and 3.6668 (17 Å].

Regio- and Enantioselective N-Allylations of Imidazole, Benzimidazole, and Purine Heterocycles Catalyzed by Single-Component Metallacyclic Iridium Complexes

Science.gov (United States)

Stanley, Levi M.

2010-01-01

Highly regio- and enantioselective iridium-catalyzed N-allylations of benzimidazoles, imidazoles, and purines have been developed. N-Allylated benzimidazoles and imidazoles were isolated in high yields (up to 97%) with high branched-to-linear selectivity (up to 99:1) and enantioselectivity (up to 98% ee) from the reactions of benzimidazole and imidazole nucleophiles with unsymmetrical allylic carbonates in the presence of single component, ethylene-bound, metallacyclic iridium catalysts. N-Allylated purines were also obtained in high yields (up to 91%) with high N9:N7 selectivity (up to 96:4), high branched-to-linear selectivity (98:2), and high enantioselectivity (up to 98% ee) under similar conditions. The reactions encompass a range of benzimidazole, imidazole, and purine nucleophiles, as well as a variety of unsymmetrical aryl, heteroaryl, and aliphatic allylic carbonates. Competition experiments between common amine nucleophiles and the heterocyclic nitrogen nucleophiles studied in this work illustrate the effect of nucleophile pKa on the rate of iridium-catalyzed N-allylation reactions. Kinetic studies on the allylation of benzimidazole catalyzed by metallacyclic iridium-phosphoramidite complexes, in combination with studies on the deactivation of these catalysts in the presence of heterocyclic nucleophiles, provide insight into the effects of the structure of the phosphoramidite ligands on the stability of the metallacyclic catalysts. The data obtained from these studies has led to the development of N-allylations of benzimidazoles and imidazoles in the absence of an exogenous base. PMID:19480431

A turn-on supramolecular fluorescent probe for sensing benzimidazole fungicides and its application in living cell imaging

Science.gov (United States)

Tang, Qing; Zhang, Jing; Sun, Tao; Wang, Cheng-Hui; Huang, Ying; Zhou, Qingdi; Wei, Gang

2018-02-01

A cucurbit[8]uril-based turn-on supramolecular fluorescent probe between cucurbit[8]uril (Q[8]) and pyronine Y (PyY) (designated 2PyY@Q[8]) in acidic aqueous solution showed a remarkable fluorescence 'turn-on' response to benzimidazole fungicides such as thiabendazole, fuberidazole and carbendazim. The 2PyY@Q[8] fluorescent probe can be used to detect benzimidazole fungicides with high sensitivity and selectivity with a detection limit of 10- 8 mol/L. A good linear relationship of emission intensity at 580 nm for benzimidazole fungicides at concentrations of 0.4-5.0 μmol/L was observed. The proposed sensing mechanism was investigated using 1H NMR spectroscopy combined with density functional theory calculations at the B3LYP/6-31G(d) level. The cell imaging study showed that the 2PyY@Q[8] complex could be used to image benzimidazole fungicide in prostate cancer (PC3) cells, which may help to elucidate relevant biological processes at the molecular level.

Synthesis, crystal structure, spectroscopic characterization, Hirshfeld surface analysis, and DFT calculations of 1,4-dimethyl-2-oxo-pyrimido[1,2-a]benzimidazole hydrate

Science.gov (United States)

El Bakri, Youness; Anouar, El Hassane; Ramli, Youssef; Essassi, El Mokhtar; Mague, Joel T.

2018-01-01

Imidazopyrimidine derivatives are organic synthesized compounds with a pyrimido[1,2-a]benzimidazole as basic skeleton. They are known for their various biological properties and as an important class of compounds in medicinal chemistry. A new 1,4-dimethyl-2-oxo-pyrimido[1,2-a]benzimidazole hydrate derivative of the tilted group has been synthesized and characterized by spectroscopic techniques NMR and FT-IR; and by a single crystal X-ray diffraction. The X-ray results showed that the tricyclic core of the title compound, C12H11N3O·H2O, is almost planar. The molecules stack along the a-axis direction in head-to- tail fashion through π-stacking interactions involving all three rings. The stacks are tied together by direct Csbnd H⋯O hydrogen bonds and by Osbnd H⋯O, Osbnd N⋯N and Csbnd H⋯O hydrogen bonds with the lattice water. DFT calculations at B3LYP/6-311++G(d,p) in gas phase an polarizable continuum model have been carried out to predict the spectral and geometrical data of the tilted compound. The obtained results showed relatively good correlations between the predicted and experimental data with correlation coefficients higher than 98%.

Regioselective Synthesis of Some Pyrazole Scaffolds Attached to Benzothiazole and Benzimidazole Moieties

Directory of Open Access Journals (Sweden)

Nabila A. Kheder

2014-01-01

Full Text Available Condensation of 2-(benzothiazol-2-ylacetonitrile (1 or 2-(1-methyl-1H-benzimidazol-2-ylacetonitrile (2 with thiophene-2-carbaldehyde afforded the corresponding acrylonitrile derivatives 3 or 4, respectively. The 1,3-dipolar cycloaddition reaction of the acrylonitrile 3 or 4 with nitrile-imine 6 gave novel pyrazole derivatives pendant to benzothiazole and benzimidazole. The pyrazoline derivative 7 was converted into the corresponding pyrazole derivative 11 via thermal elimination of hydrogen cyanide upon heating in sodium ethoxide solution. The structures of the synthesized products were confirmed by IR, 1H NMR, and mass spectral techniques.

Synthesis, pharmacological activity evaluation and molecular modeling of new polynuclear heterocyclic compounds containing benzimidazole derivatives.

Science.gov (United States)

Bassyouni, Fatma A; Saleh, Tamer S; ElHefnawi, Mahmoud M; Abd El-Moez, Sherein I; El-Senousy, Waled M; Abdel-Rehim, Mohamed E

2012-12-01

Novel heterocyclic compounds containing benzimidazole derivatives were synthesized from 2-(1H-benzimidazol-2-yl) acetonitrile (1) and arylhydrazononitrile derivative 2 was obtained via coupling of 1 with 4-methyl phenyldiazonium salt, which was then reacted with hydroxylamine hydrochloride to give amidooxime derivative 3. This product was cyclized into the corresponding oxadiazole derivative 4 upon reflux in acetic anhydride. Compound 4 was refluxed in DMF in the presence of triethylamine to give the corresponding 5-(1H-benzimidazol-2-yl)-2-p-tolyl-2H-1,2,3-triazol-4-amine 6. Treatment of compound 6 with ethyl chloroformate afforded 2,6-dihydro-2-(4-methylphenyl)-1,2,3-triazolo[4",5"-4',5']pyrimido[1,6-a]benzimidazole-5(4H)-one (8). 1,2-bis(2-cyanomethyl-1H-benzimidazol-1-yl)ethane-1,2-dione (10) was synthesized via the condensation reaction of 2-(1H-benzimidazol-2-yl) acetonitrile (1) and diethyloxalate. The reactivity of compound 10 towards some diamine reagents was studied. The in vitro antimicrobial activity of the synthesized compounds was investigated against several pathogenic bacterial strains such as Escherichia coli O157, Salmonella typhimurium, E. coli O119, S. paratyphi, Pseudomonas aeruginosa, Staphylococcus aureus, Listeria monocytogenes and Bacillus cereus. The results of MIC revealed that compounds 12a-c showed the most effective antimicrobial activity against tested strains. On the other hand, compounds 12a, b exhibited high activity against rotavirus Wa strain while compounds 12b, c exhibited high activity against adenovirus type 7. In silico target prediction, docking and validation of the compounds 12a-c were performed. The dialkylglycine decarboxylase bacterial enzyme was predicted as a potential bacterial target receptor using pharmacophore-based correspondence with previous leads; giving the highest normalized scores and a high correlation docking score with mean inhibition concentrations. A novel binding mechanism was predicted after docking

Laser assisted anticancer activity of benzimidazole based metal organic nanoparticles.

Science.gov (United States)

Praveen, P A; Ramesh Babu, R; Balaji, P; Murugadas, A; Akbarsha, M A

2018-03-01

Recent studies showed that the photothermal therapy can be effectively used for the targeted cancerous cells destruction. Hence, in the present study, benzimidazole based metal organic complex nanoparticles, dichloro cobalt(II) bis-benzimidazole (Co-BMZ) and dichloro copper(II) bis-benzimidazole (Cu-BMZ), were synthesized by reprecipitation method and their anti-cancer activity by means of photothermal effect has been studied. Transmission electron microscopy analysis shows that the particle size of Cu-BMZ is ∼100 nm and Co-BMZ is in the range between 100 and 400 nm. Zeta potential analysis ensures the stability of the synthesized nanoparticles. It is found that the nonlinear absorption of the nanoparticles increases with increase in laser power intensity. Phototoxicity of human lung cancer (A549) and the normal mouse embryonic fibroblast (NIH-3T3) cells was studied using a 650 nm laser. Even though both the cell lines were affected by laser irradiation, A549 cells show higher cell destruction and lower IC 50 values than the normal cells. Docking studies were used to analyse the interaction site and the results showed that the Cu-BMZ molecules have higher dock score than the Co-BMZ molecules. The obtained results indicate that Cu-BMZ samples have lesser particle size, higher nonlinear absorption and higher interaction energy than the Co-BMZ samples. Copyright © 2018 Elsevier B.V. All rights reserved.

A ring system detected around the Centaur (10199) Chariklo.

Science.gov (United States)

Braga-Ribas, F; Sicardy, B; Ortiz, J L; Snodgrass, C; Roques, F; Vieira-Martins, R; Camargo, J I B; Assafin, M; Duffard, R; Jehin, E; Pollock, J; Leiva, R; Emilio, M; Machado, D I; Colazo, C; Lellouch, E; Skottfelt, J; Gillon, M; Ligier, N; Maquet, L; Benedetti-Rossi, G; Ramos Gomes, A; Kervella, P; Monteiro, H; Sfair, R; El Moutamid, M; Tancredi, G; Spagnotto, J; Maury, A; Morales, N; Gil-Hutton, R; Roland, S; Ceretta, A; Gu, S-h; Wang, X-b; Harpsøe, K; Rabus, M; Manfroid, J; Opitom, C; Vanzi, L; Mehret, L; Lorenzini, L; Schneiter, E M; Melia, R; Lecacheux, J; Colas, F; Vachier, F; Widemann, T; Almenares, L; Sandness, R G; Char, F; Perez, V; Lemos, P; Martinez, N; Jørgensen, U G; Dominik, M; Roig, F; Reichart, D E; LaCluyze, A P; Haislip, J B; Ivarsen, K M; Moore, J P; Frank, N R; Lambas, D G

2014-04-03

Hitherto, rings have been found exclusively around the four giant planets in the Solar System. Rings are natural laboratories in which to study dynamical processes analogous to those that take place during the formation of planetary systems and galaxies. Their presence also tells us about the origin and evolution of the body they encircle. Here we report observations of a multichord stellar occultation that revealed the presence of a ring system around (10199) Chariklo, which is a Centaur--that is, one of a class of small objects orbiting primarily between Jupiter and Neptune--with an equivalent radius of 124 ±  9 kilometres (ref. 2). There are two dense rings, with respective widths of about 7 and 3 kilometres, optical depths of 0.4 and 0.06, and orbital radii of 391 and 405 kilometres. The present orientation of the ring is consistent with an edge-on geometry in 2008, which provides a simple explanation for the dimming of the Chariklo system between 1997 and 2008, and for the gradual disappearance of ice and other absorption features in its spectrum over the same period. This implies that the rings are partly composed of water ice. They may be the remnants of a debris disk, possibly confined by embedded, kilometre-sized satellites.

Quantized levitation states of superconducting multiple-ring systems

International Nuclear Information System (INIS)

Haley, S.B.; Fink, H.J.

1996-01-01

The quantized levitation, trapped, and suspension states of a magnetic microsphere held in equilibrium by two fixed superconducting (SC) microrings are calculated by minimizing the free energy of the system. Each state is a discrete function of two independent fluxoid quantum numbers of the rings. When the radii of the SC rings are of the same order as the Ginzburg-Landau coherence length ξ(T), the system exhibits a small set of gravity and temperature-dependent levels. The levels of a weakly magnetized particle are sensitive functions of the gravitational field, indicating potential application as an accelerometer, and for trapping small magnetic particles in outer space or on Earth. The equilibrium states of a SC ring levitated by another SC ring are also calculated. copyright 1996 The American Physical Society

Polybenzimidazole Membranes Containing Benzimidazole Side Groups for High Temprature Polymer Electrolyte Membrane Fuel Cells

DEFF Research Database (Denmark)

Yang, Jingshuai; Li, Xueyuan; Xu, Yizin

2013-01-01

Polybenzimidazole (PBI) with a high molecular weight of 69,000 was first synthesized. It was afterwards grafted with benzimidazole pendant groups on the backbones. The acid doped benzimidaozle grafted PBI membranes were investigated and characterized including fuel cell tests at elevated temperat......Polybenzimidazole (PBI) with a high molecular weight of 69,000 was first synthesized. It was afterwards grafted with benzimidazole pendant groups on the backbones. The acid doped benzimidaozle grafted PBI membranes were investigated and characterized including fuel cell tests at elevated...... temperatures without humidification. At an acid doping level of 13.1 mol H3PO4 per average molar repeat unit, the PBI membranes with a benzimidazole grafting degree of 10.6% demonstrated a conductivity of 0.15 S cm-1 and a H2-air fuel cell peak power density of 378 mW cm-2 at 180 oC at ambient pressure without...

O-Ring sealing arrangements for ultra-high vacuum systems

Science.gov (United States)

Kim, Chang-Kyo; Flaherty, Robert

1981-01-01

An all metal reusable O-ring sealing arrangement for sealing two concentric tubes in an ultra-high vacuum system. An O-ring of a heat recoverable alloy such as Nitinol is concentrically positioned between protruding sealing rings of the concentric tubes. The O-ring is installed between the tubes while in a stressed martensitic state and is made to undergo a thermally induced transformation to an austenitic state. During the transformation the O-ring expands outwardly and contracts inwardly toward a previously sized austenitic configuration, thereby sealing against the protruding sealing rings of the concentric tubes.

Ball Milling Assisted Solvent and Catalyst Free Synthesis of Benzimidazoles and Their Derivatives.

Science.gov (United States)

El-Sayed, Taghreed H; Aboelnaga, Asmaa; Hagar, Mohamed

2016-08-24

Benzoic acid and o-phenylenediamine efficiently reacted under the green solvent-free Ball Milling method. Several reaction parameters were investigated such as rotation frequency; milling balls weight and milling time. The optimum reaction condition was milling with 56.6 g weight of balls at 20 Hz frequency for one hour milling time. The study was extended for synthesis of a series of benzimidazol-2-one or benzimidazol-2-thione using different aldehydes; carboxylic acids; urea; thiourea or ammonium thiocyanate with o-phenylenediamine. Moreover; the alkylation of benzimidazolone or benzimidazolthione using ethyl chloroacetate was also studied.

Light fluorous-tagged traceless one-pot synthesis of benzimidazoles facilitated by microwave irradiation.

Science.gov (United States)

Tseng, Chih-Chung; Tasi, Cheng-Hsun; Sun, Chung-Ming

2012-06-01

A novel protocol for rapid assemble of benzimidazole framework has been demonstrated. This method incorporated with light fluorous-tag provides a convenient method for diversification of benzimidazoles and for easy purification via fluorous solid-phase extraction (F-SPE) in a parallel manner. The key transformation of this study involves in situ reduction of aromatic nitro compound, amide formation, cyclization and aromatization promoted by microwave irradiation in a one-pot fashion. The strategy is envisaged to be applied for the establishment of drug-like small molecule libraries for high throughput screening.

1-Hydroxyethyl-2-Substituted Phenoxymethyl Benzimidazoles: Synthesis and Crystal Structures

International Nuclear Information System (INIS)

Wu, J.; Wang, Z.; Gu, H.; Chen, W.; Zhao, L.; Zhao, C.

2016-01-01

Five novel 1-hydroxyethyl-2-substituted phenoxymethyl benzimidazoles c1-c5 were successfully synthesized by a three-step route. Firstly, five substituted phenoxymethyl acids a1-a5 were prepared by the O-carboxymethylation reaction of the starting substituted phenols under microwave irradiation. Then, these compounds reacted with o-phenylendiamine to get the key intermediates 2-substituted phenoxymethyl benzimidazoles b1-b5. At last, the target compounds were synthesized by the N-hydroxyethylation reaction of b1-b5 with 2-chloroethyl alcohol through the solid-liquid phase transfer catalysis method, where tetrabutyl ammonium bromide (TBAB) was used as the catalyst. The structures of the target compounds were well characterized and verified by elemental analysis, MS, IR, 1H NMR, 13C NMR and single crystal X-ray diffraction analysis. (author)

The Influence of Substituents on the Tautomerism of Symmetrically Substituted 2,2'-Bis-benzimidazoles

Directory of Open Access Journals (Sweden)

Dall'Oglio Evandro

2002-01-01

Full Text Available The tautomerism of five symmetrically substituted 2,2'-bis-benzimidazoles [5(6,5'(6'-tetramethyl- (1; 5(6,5'(6'-dimethyl-(2; 5(6,5'(6'-dichloro- (3; 5(6,5'(6'-dimethoxy- (4 and 4(7,4'(7'-dimethyl-2,2'-bis-benzimidazole (5], was studied by means of ¹H NMR spectroscopy at variable temperatures, and the influence of the substituents on the energy barriers for tautomeric interconversion was interpreted with the aid of theoretical calculations.

Improvement of surface wettability and interfacial adhesion of poly-(p-phenylene terephthalamide) by incorporation of the polyamide benzimidazole segment

International Nuclear Information System (INIS)

Cai Renqin; Peng Tao; Wang Fengde; Ye Guangdou; Xu Jianjun

2011-01-01

In order to investigate the effect of the polyamide benzimidazole group on the surface wettability and interfacial adhesion of fiber/matrix composites, surface features of two kinds of aramid fibers, poly (p-phenylene terephthalamide) fiber (Kevlar-49) and poly-(polyamide benzimidazole-co-p-phenylene terephthalamide) (DAFIII), have been analyzed by X-ray photoelectron spectroscopy (XPS), scanning electron microscopy (SEM) and contact angle analysis (CAA) system, respectively. The results show that with the incorporation of the polyamide benzimidazole segment, more polar functional groups exist on DAFIII surface. The contact angles of water and diiodomethane on DAFIII surface get smaller. The surface free energy of DAFIII increases to 36.5 mJ/m 2 , which is 2.3% higher than that of Kevlar-49. In addition, DAFIII has a larger rough surface compared with that of Kevlar-49 due to different spinning processes. The interfacial shear strength (IFSS) of DAFIII/matrix composite is 25.7% higher than that of Kevlar-49/matrix composite, in agreement with the observed results from surface feature tests. SEM micrographs of failed micro-droplet specimens reveal a strong correlation between the fracture features and the observed test data.

The mechanism of transition-metal (Cu or Pd)-catalyzed synthesis of benzimidazoles from amidines: theoretical investigation.

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Li, Juan; Gu, Honghong; Wu, Caihong; Du, Lijuan

2014-11-28

In this study, the Cu(OAc)2- and [PdCl2(PhCN)2]-catalyzed syntheses of benzimidazoles from amidines were theoretically investigated using density functional theory calculations. For the Cu-catalyzed system, our calculations supported a four-step-pathway involving C-H activation of an arene with Cu(II) via concerted metalation-deprotonation (CMD), followed by oxidation of the Cu(II) intermediate and deprotonation of the imino group by Cu(III), and finally reductive elimination from Cu(III). In our calculations, the barriers for the CMD step and the oxidation step are the same. The results are different from the ones reported by Fu et al. in which the whole reaction mechanism includes three steps and the CMD step is rate determining. On the basis of the calculation results for the [PdCl2(PhCN)2]-catalyzed system, C-H bond breaking by CMD occurs first, followed by the rate-determining C-N bond formation and N-H deprotonation. Pd(III) species is not involved in the [PdCl2(PhCN)2]-catalyzed syntheses of benzimidazoles from amidines.

Discovery of a novel series of benzimidazole derivatives as diacylglycerol acyltransferase inhibitors.

Science.gov (United States)

Lee, Kyeong; Goo, Ja-Il; Jung, Hwa Young; Kim, Minkyoung; Boovanahalli, Shanthaveerappa K; Park, Hye Ran; Kim, Mun-Ock; Kim, Dong-Hyun; Lee, Hyun Sun; Choi, Yongseok

2012-12-15

A novel series of benzimidazole derivatives was prepared and evaluated for their diacylglycerol acyltransferase (DGAT) inhibitory activity using microsome from rat liver. Among the newly synthesized compounds, furfurylamine containing benzimidazole carboxamide 10j showed the most potent DGAT inhibitory effect (IC(50)=4.4 μM) and inhibited triglyceride formation in HepG2 cells. Furthermore, compound 10j reduced body weight gain of Institute of Cancer Research mice on a high-fat diet and decreased levels of total triglyceride, total cholesterol, and LDL-cholesterol in the blood accompanied with a significant increase in HDL-cholesterol level. Copyright © 2012 Elsevier Ltd. All rights reserved.

Thermodynamics of formation of cadmium dicarboxylate and carboxylate mixed complexes with benzimidazole

Energy Technology Data Exchange (ETDEWEB)

Kharitonov, G V; Bolotov, V M; Kharitonova, R I [Voronezhskij Tekhnologicheskij Inst. (USSR)

1980-01-01

Thermodynamic parameters of the mixed complexing of cadmium propionate, butyrate, valerate, succinate, maleinate and malate with benzimidazole in 20 % aqUeous-ethanol solution of 0.1 M KNO/sub 3/ are studied using polarographic method. It is shown that stability of mixed complexes of cadmium carboxylates with benzimidazole is connected with the process enthalpy and is determined by covalency of the metal-carboxylate bond. Increasing length of hydrocarbon chain of acyl group of monobasic acids hampers amine coordination with central complexing agent (..delta..S<0). The presence of dicarboxylate-ion in the inner coordination sphere decreases the enthalpy and increases the entropy of the process (..delta..S>0).

Benzimidazole acrylonitriles as multifunctional push-pull chromophores: Spectral characterisation, protonation equilibria and nanoaggregation in aqueous solutions

Science.gov (United States)

Horak, Ema; Vianello, Robert; Hranjec, Marijana; Krištafor, Svjetlana; Zamola, Grace Karminski; Steinberg, Ivana Murković

2017-05-01

Heterocyclic donor-π-acceptor molecular systems based on an N,N-dimethylamino phenylacrylonitrile benzimidazole skeleton have been characterised and are proposed for potential use in sensing applications. The benzimidazole moiety introduces a broad spectrum of useful multifunctional properties to the system including electron accepting ability, pH sensitivity and compatibility with biomolecules. The photophysical characterisation of the prototropic forms of these chromophores has been carried out in both solution and on immobilisation in polymer films. The experimental results are further supported by computational determination of pKa values. It is noticed that compound 3 forms nanoaggregates in aqueous solutions with aggregation-induced emission (AIE) at 600 nm. All the systems demonstrate spectral pH sensitivity in acidic media which shifts towards near-neutral values upon immobilisation in polymer films or upon aggregation in an aqueous environment (compound 3). The structure-property relationships of these functional chromophores, involving their spectral characteristics, acid-base equilibria, pKa values and aggregation effects have been determined. Potential applications of the molecules as pH and biomolecular sensors are proposed based on their pH sensitivity and AIE properties.

Benzimidazoles: an ideal privileged drug scaffold for the design of multitargeted anti-inflammatory ligands.

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Kaur, Gaganpreet; Kaur, Maninder; Silakari, Om

2014-01-01

The recent research area endeavors to discover ultimate multi-target ligands, an increasingly feasible and attractive alternative to existing mono-targeted drugs for treatment of complex, multi-factorial inflammation process which underlays plethora of debilitated health conditions. In order to improvise this option, exploration of relevant chemical core scaffold will be an utmost need. Privileged benzimidazole scaffold being historically versatile structural motif could offer a viable starting point in the search for novel multi-target ligands against multi-factorial inflammation process since, when appropriately substituted, it can selectively modulate diverse receptors, pathways and enzymes associated with the pathogenesis of inflammation. Despite this remarkable capability, the multi-target capacity of the benzimidazole scaffold remains largely unexploited. With this in focus, the present review article attempts to provide synopsis of published research to exemplify the valuable use of benzimidazole nucleus and focus on their suitability as starting scaffold to develop multi-targeted anti-inflammatory ligands.

Design, synthesis, α-glucosidase inhibitory activity, molecular docking and QSAR studies of benzimidazole derivatives

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Dinparast, Leila; Valizadeh, Hassan; Bahadori, Mir Babak; Soltani, Somaieh; Asghari, Behvar; Rashidi, Mohammad-Reza

2016-06-01

In this study the green, one-pot, solvent-free and selective synthesis of benzimidazole derivatives is reported. The reactions were catalyzed by ZnO/MgO containing ZnO nanoparticles as a highly effective, non-toxic and environmentally friendly catalyst. The structure of synthesized benzimidazoles was characterized using spectroscopic technics (FT-IR, 1HNMR, 13CNMR). Synthesized compounds were evaluated for their α-glucosidase inhibitory potential. Compounds 3c, 3e, 3l and 4n were potent inhibitors with IC50 values ranging from 60.7 to 168.4 μM. In silico studies were performed to explore the binding modes and interactions between enzyme and synthesized benzimidazoles. Developed linear QSAR model based on density and molecular weight could predict bioactivity of newly synthesized compounds well. Molecular docking studies revealed the availability of some hydrophobic interactions. In addition, the bioactivity of most potent compounds had good correlation with estimated free energy of binding (ΔGbinding) which was calculated according to docked best conformations.

Zirconyl (IV Nitrate as Efficient and Reusable Solid Lewis Acid Catalyst for the Synthesis of Benzimidazole Derivatives

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Pratapsinha B. Gorepatil

2013-01-01

Full Text Available The present paper introduces a simple and efficient method for the synthesis of substituted benzimidazoles by heterocyclization of different o-phenylenediamines and substituted aromatic carboxylic acid/aldehyde in the presence of zirconyl nitrate as catalyst in ethanol under reflux, which produced excellent yield of corresponding benzimidazoles in a short reaction time with reusability of catalyst.

An Automatic Assembling System for Sealing Rings Based on Machine Vision

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Mingyu Gao

2017-01-01

Full Text Available In order to grab and place the sealing rings of battery lid quickly and accurately, an automatic assembling system for sealing rings based on machine vision is developed in this paper. The whole system is composed of the light sources, cameras, industrial control units, and a 4-degree-of-freedom industrial robot. Specifically, the sealing rings are recognized and located automatically with the machine vision module. Then industrial robot is controlled for grabbing the sealing rings dynamically under the joint work of multiple control units and visual feedback. Furthermore, the coordinates of the fast-moving battery lid are tracked by the machine vision module. Finally the sealing rings are placed on the sealing ports of battery lid accurately and automatically. Experimental results demonstrate that the proposed system can grab the sealing rings and place them on the sealing port of the fast-moving battery lid successfully. More importantly, the proposed system can improve the efficiency of the battery production line obviously.

Effect of benzimidazol-derivatives on the DNA-protein binding formation after UV-radiation of chromatin

International Nuclear Information System (INIS)

Mil', E.M.; Binyukov, V.I.; Zhil'tsova, V.M.; Stolyarova, L.G.; Kuznetsov, Yu.V.

1991-01-01

Effect of benzimidazol-derivatives on the DNA-protein binding formation was studied after UV-radiation of chromatin. These derivatives were shown to protect chromatin from UV-induced DNA-protein binding formation. Structural analog contained two aminomethyl residuals sensibilized additional binding formation in chromatin. Results suggested, that benzimidazol interacted with DNA, while aminomethyl groups interacted with protein and sensibilized binding of DNA, whilt aminomethyl groups interacted with protein and sensibilized binding of DNA with histone H1

Halide/pseudohalide complexes of cadmium(II) with benzimidazole: Synthesis, crystal structures and fluorescence properties

Science.gov (United States)

Zhao, Hai-Yan; Yang, Fu-Li; Li, Na; Wang, Xiao-Jing

2017-11-01

Two new dinuclear Cd(II) complexes, [CdL1Cl2]2·H2O (1) and [CdL1(N3)2]2·CH3OH (2) and one dicyanamide bridged one-dimensional polynuclear network [CdL1(μ1,5-dca)dca]n (3) of the potentially tridentate NNN-donor Schiff base 2-((1H-benzimidazol-2-yl-ethylimino)-methyl)pyridine (L1) and another dinucler Cd(II) complex [CdL2Cl(dca)]2 (4) of a similar NNN-donor Schiff base ligand 2-((1H-benzimidazol-2-yl-propylimino)-methyl)pyridine (L2), have been synthesized and characterized by elemental analyses, IR and single crystal X-ray crystallography. The ligands L1 and L2 are [1 + 1] condensation products of pyridine-2-carbaldehyde with 2-aminoethyl-1H-benzimidazole and 2-aminopropyl-1H-benzimidazole, respectively. In the complexes 1 and 4 the two Cd(II) centers are held together by the bridged chloride ligands, while in 2 the two Cd(II) centers are bridged by μ1,1-azide ions. Complex 3 has a one-dimensional infinite chain structure in which Cd(II) ions are bridged by single dicyanamide groups in end-to-end fashion. All the metal centers have a distorted octahedral geometry and H-bonding or π⋯π interactions are operative to bind the complex units in the solid state. Furthermore, these complexes have been investigated by thermogravimetric analyses and fluorescence spectra.

99mTc complexes of benzimidazole and benzoxazole ligands and their biodistribution studies

International Nuclear Information System (INIS)

Kothari, K.; Manju, S.; Pillai, M.R.A.; Rath, N.; Dash, K.C.; Sarma, H.D.

1997-01-01

Complexation studies of 2 (2' -hydroxyphenyl)benzimidazole (HPBI) and 2(2' -pyridyl)benzoxazole (PBO) with 99m Tc were carried out. The complexes were characterised by TLC, paper electrophoresis and solvent extraction. The ligand HPBI forms complex in high yield (>90%). Biodistribution studies carried out with 99m Tc-HPBI complex in Swiss Albino mice showed rapid clearance of the complex from blood and excretion of the activity through hepatobiliary system. (author). 2 refs., 1 fig., 3 tabs

A trisubstituted benzimidazole cell division inhibitor with efficacy against Mycobacterium tuberculosis.

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Susan E Knudson

Full Text Available Trisubstituted benzimidazoles have demonstrated potency against Gram-positive and Gram-negative bacterial pathogens. Previously, a library of novel trisubstituted benzimidazoles was constructed for high throughput screening, and compounds were identified that exhibited potency against M. tuberculosis H37Rv and clinical isolates, and were not toxic to Vero cells. A new series of 2-cyclohexyl-5-acylamino-6-N, N-dimethylaminobenzimidazoles derivatives has been developed based on SAR studies. Screening identified compounds with potency against M. tuberculosis. A lead compound from this series, SB-P17G-A20, was discovered to have an MIC of 0.16 µg/mL and demonstrated efficacy in the TB murine acute model of infection based on the reduction of bacterial load in the lungs and spleen by 1.73 ± 0.24 Log10 CFU and 2.68 ± Log10 CFU, respectively, when delivered at 50 mg/kg by intraperitoneal injection (IP twice daily (bid. The activity of SB-P17G-A20 was determined to be concentration dependent and to have excellent stability in mouse and human plasma, and liver microsomes. Together, these studies demonstrate that SB-P17G-A20 has potency against M. tuberculosis clinical strains with varying susceptibility and efficacy in animal models of infection, and that trisubstituted benzimidazoles continue to be a platform for the development of novel inhibitors with efficacy.

A Trisubstituted Benzimidazole Cell Division Inhibitor with Efficacy against Mycobacterium tuberculosis

Science.gov (United States)

Knudson, Susan E.; Awasthi, Divya; Kumar, Kunal; Carreau, Alexandra; Goullieux, Laurent; Lagrange, Sophie; Vermet, Hélèn; Ojima, Iwao; Slayden, Richard A.

2014-01-01

Trisubstituted benzimidazoles have demonstrated potency against Gram-positive and Gram-negative bacterial pathogens. Previously, a library of novel trisubstituted benzimidazoles was constructed for high throughput screening, and compounds were identified that exhibited potency against M. tuberculosis H37Rv and clinical isolates, and were not toxic to Vero cells. A new series of 2-cyclohexyl-5-acylamino-6-N, N-dimethylaminobenzimidazoles derivatives has been developed based on SAR studies. Screening identified compounds with potency against M. tuberculosis. A lead compound from this series, SB-P17G-A20, was discovered to have an MIC of 0.16 µg/mL and demonstrated efficacy in the TB murine acute model of infection based on the reduction of bacterial load in the lungs and spleen by 1.73±0.24 Log10 CFU and 2.68±Log10 CFU, respectively, when delivered at 50 mg/kg by intraperitoneal injection (IP) twice daily (bid). The activity of SB-P17G-A20 was determined to be concentration dependent and to have excellent stability in mouse and human plasma, and liver microsomes. Together, these studies demonstrate that SB-P17G-A20 has potency against M. tuberculosis clinical strains with varying susceptibility and efficacy in animal models of infection, and that trisubstituted benzimidazoles continue to be a platform for the development of novel inhibitors with efficacy. PMID:24736743

Fano and Dicke effects in a double Rashba-ring system

International Nuclear Information System (INIS)

Apel, V M; Orellana, P A; Pacheco, M

2008-01-01

The electronic transport in a system of two quantum rings side-coupled to a quantum wire is studied via a single-band tunneling tight-binding Hamiltonian. We derived analytical expressions for the conductance and spin polarization when the rings are threaded by magnetic fluxes with Rashba spin-orbit interaction. We show that by using the Fano and Dicke effects this system can be used as an efficient spin filter even for small spin-orbit interaction and small values of magnetic fluxes. We compare the spin-dependent polarization of this design and the polarization obtained with one ring side-coupled to a quantum ring. As a main result, we find better spin polarization capabilities as compared to the one-ring design

An Efficient Synthesis of 2-Substituted Benzimidazoles via Photocatalytic Condensation of o-Phenylenediamines and Aldehydes.

Science.gov (United States)

Kovvuri, Jeshma; Nagaraju, Burri; Kamal, Ahmed; Srivastava, Ajay K

2016-10-10

A photocatalytic method has been developed for the efficient synthesis of functionalized benzimidazoles. This protocol involves photocatalytic condensation of o-phenylenediamines with various aldehydes using the Rose Bengal as photocatalyst. The method was found to be general and was successfully employed for accessing pharmaceutically important benzimidazoles by the condensation of aromatic, heteroaromatic and aliphatic aldehydes with o-phenylenediamines, in good-to-excellent yields. Notably, the method was found to be effective for the condensation of less reactive heterocyclic aldehydes with o-phenylenediamines.

CORRECTION SYSTEMS UPGRADE FOR THE SNS RING

International Nuclear Information System (INIS)

PAPAPHILIPPOU, Y.; GARDNER, C.J.; LEE, Y.Y.; WEI, J.

2001-01-01

In view of the changes in the design of the SNS ring from the original FODO lattice [l] to the 220m hybrid lattice [2] and finally 1.3GeV compatible 248m ring [3], complementary studies have been undertaken, in order to upgrade its correction packages. We review the evolution of the correction systems and present the accelerator physics studies for the adopted schemes and powering plan

Conjugation of Benzylvanillin and Benzimidazole Structure Improves DNA Binding with Enhanced Antileukemic Properties

Science.gov (United States)

Al-Mudarris, Ban A.; Chen, Shih-Hsun; Liang, Po-Huang; Osman, Hasnah; Jamal Din, Shah Kamal Khan; Abdul Majid, Amin M. S.

2013-01-01

Benzyl-o-vanillin and benzimidazole nucleus serve as important pharmacophore in drug discovery. The benzyl vanillin (2-(benzyloxy)-3-methoxybenzaldehyde) compound shows anti-proliferative activity in HL60 leukemia cancer cells and can effect cell cycle progression at G2/M phase. Its apoptosis activity was due to disruption of mitochondrial functioning. In this study, we have studied a series of compounds consisting of benzyl vanillin and benzimidazole structures. We hypothesize that by fusing these two structures we can produce compounds that have better anticancer activity with improved specificity particularly towards the leukemia cell line. Here we explored the anticancer activity of three compounds namely 2-(2-benzyloxy-3-methoxyphenyl)-1H-benzimidazole, 2MP, N-1-(2-benzyloxy-3-methoxybenzyl)-2-(2-benzyloxy-3-methoxyphenyl)-1H-benzimidazole, 2XP, and (R) and (S)-1-(2-benzyloxy-3-methoxyphenyl)-2, 2, 2-trichloroethyl benzenesulfonate, 3BS and compared their activity to 2-benzyloxy-3-methoxybenzaldehyde, (Bn1), the parent compound. 2XP and 3BS induces cell death of U937 leukemic cell line through DNA fragmentation that lead to the intrinsic caspase 9 activation. DNA binding study primarily by the equilibrium binding titration assay followed by the Viscosity study reveal the DNA binding through groove region with intrinsic binding constant 7.39 µM/bp and 6.86 µM/bp for 3BS and 2XP respectively. 2XP and 3BS showed strong DNA binding activity by the UV titration method with the computational drug modeling showed that both 2XP and 3BS failed to form any electrostatic linkages except via hydrophobic interaction through the minor groove region of the nucleic acid. The benzylvanillin alone (Bn1) has weak anticancer activity even after it was combined with the benzimidazole (2MP), but after addition of another benzylvanillin structure (2XP), stronger activity was observed. Also, the combination of benzylvanillin with benzenesulfonate (3BS) significantly improved the

Effect of chemicals (benzimidazole, methyl thiophanate and potassium) in reducing ozone injury to vegetable crops

Energy Technology Data Exchange (ETDEWEB)

Shibukawa, S; Ota, Y

1973-01-01

Following the previous report on the effect of methyl thiophanate for reducing the damages of photochemical oxidants on agricultural produce, effective concentrations and time factors were studied, and the results were compared with that of benzimidazole. Spinach and radishes were grown in pots, and 21, 11, 6, and 3 days prior to ozone exposure tests, 6.25-100 micrograms of benzimidazole and 77.5-310 micrograms of methyl thiophanate solutions were injected into the various pot soils. Exposure to 0.25 ppm O/sub 3/ was given for four hours to spinach and for 2.5 hours to radishes. In all cases, benzimidazole showed a remarkable effect on reducing the damages of O/sub 3/, especially when injected 5-11 days prior to the exposure. Methyl thiophanate was very effective for radishes but had no effect on spinach. Whether this was due to an insufficient amount of chemicals or due to its selectivity is not clear at this stage of the experiments.

Effect of substituted benzimidazoles on acid secretion in isolated and enriched guinea pig parietal cells.

Science.gov (United States)

Sewing, K F; Harms, P; Schulz, G; Hannemann, H

1983-01-01

The inhibitory effect of the three benzimidazole derivatives timoprazole, picoprazole, and omeprazole on histamine and dbcAMP stimulated 14C-aminopyrine accumulation (= H+ secretion) has been studied in isolated and enriched guinea-pig parietal cells. All compounds tested inhibited H+ secretion in a concentration dependent manner with IC50 values of 8.5 +/- 1.9 mumol/l for timoprazole, 3.9 +/- 0.7 mumol/l for picoprazole, and 0.13 +/- 0.03 mumol/l for omeprazole. The IC50 of timoprazole, when dbcAMP was used as a stimulus, did not differ significantly from that of histamine stimulation. The type of inhibition was of a non-competitive nature. The full acid response to histamine after temporary exposure of the cells to the benzimidazoles could be restored by washing the cells twice; this suggests that the inhibition is reversible. The data - among others - indicate that the properties of the benzimidazoles described here would allow these compounds to be used as effective antisecretagogues. PMID:6303916

Synthesis and in Vitro Antiproliferative Evaluation of Some B-norcholesteryl Benzimidazole and Benzothiazole Derivatives

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Jianguo Cui

2015-04-01

Full Text Available Taking orostanal (a compound from a Japanese marine sponge, Stelletta hiwasaensis as a lead compound, some novel B-norcholesteryl benzimidazole and benzothiazole derivatives were synthesized. The antiproliferative activity of the compounds against human cervical carcinoma (HeLa, human lung carcinoma (A549, human liver carcinoma cells (HEPG2 and normal kidney epithelial cells (HEK293T was assayed. The results revealed that the benzimidazole group was a better substituent than benzothiazole group for increasing the antiproliferative activity of compounds. 2-(3β′-Acetoxy-5β′-hydroxy-6′-B-norcholesterylbenzimidazole (9b with the structure of 6-benzimidazole displays the best antiproliferative activity to the cancer cells in all compounds, but is almost inactive to normal kidney epithelial cells (HEK293T. The assay of compound 9b to cancer cell apoptosis by flow cytometry showed that the compound was able to effectively induce cancer cell apoptosis. The research provided a theoretical reference for the exploration of new anti-cancer agents and may be useful for the design of novel chemotherapeutic drugs.

Investigation of REE perchlorates complexing with benzimidazole in aqua-dioxane media

International Nuclear Information System (INIS)

Akhrimenko, Z.M.; Panyushkin, V.T.; Ishbulatova, S.K.

1992-01-01

Stability constant (K 1 ) of complexes of rare earth perchlorates with benzimidazole were determined by the method of pH-metric titration. Nonmonotonous change in lgK 1 with rare earth ordinal number increase was revealed

Benzimidazoles and benzoxazoles via the nucleophilic addition of anilines to nitroalkanes.

Science.gov (United States)

Aksenov, Alexander V; Smirnov, Alexander N; Aksenov, Nicolai A; Bijieva, Asiyat S; Aksenova, Inna V; Rubin, Michael

2015-04-14

PPA-induced umpolung triggers efficient nucleophilic addition of unactivated anilines to nitroalkanes to produce N-hydroxyimidamides. The latter undergo sequential acid-promoted cyclocondensation with ortho-OH or ortho-NHR moieties to afford benzoxazoles and benzimidazoles, respectively.

Synthesis of benzimidazoles by PIDA-promoted direct C(sp2)-H imidation of N-arylamidines.

Science.gov (United States)

Huang, Jinbo; He, Yimiao; Wang, Yong; Zhu, Qiang

2012-10-29

A metal-free synthesis of diversified benzimidazoles from N-arylamidines through a phenyliodine(III) diacetate (PIDA) promoted intramolecular direct C(sp(2))-H imidation has been developed. The reaction proceeds smoothly at 0 °C or ambient temperature to provide the desired products in good to excellent yields. The synthesis of 2-alkyl- or 2-alkyl-fused benzimidazoles, which are generally inaccessible by similar Pd- or Cu-catalyzed approaches, can also be achieved. Copyright © 2012 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

The injection system of the stretcher ring ELSA

International Nuclear Information System (INIS)

Dreist, A.

1989-07-01

For the stretcher ring ELSA in the framwork of this thesis an injection system has been concipated and constructed which should allow all projected operational modes of this stretcher ring, the stretcher, the post-acceleration, and the accumulation mode. The proof could be performed that the realized concept allows all these operational modes. Furthermore it could be shown that the injection shifted from the equilibrium orbit has no disadvantageous effects on a uniform extraction and by this on a high touching ratio. In fact it is even possible to apply the decay of the coherent betatron oscillations around the equilibrium orbit, caused by injection of the incident beam shifted from the equilibrium orbit, to diagnosis purposes: By reproduction of this damping process in a simulation model statements on nonlinearities present in the ring and by this statements on the actual phase-space structure are possible. It has so been shown that the concept presented in this thesis and realized for this thesis represents a suited injection system for the stretcher ring ELSA. (orig.) [de

Synthesis and molecular structures of 1-hydroxyethyl-2-(p-substituted) phenoxymethyl benzimidazoles

International Nuclear Information System (INIS)

Wu, J.W.; Zhao, L.; Wang, Z.; Gu, H.; Chen, W.; Zhao, C.

2016-01-01

Five novel 1-hydroxyethyl-2-(p-substituted) phenoxymethyl benzimidazoles were synthesized by a three-step route. Under microwave irradiation, the p-substituted phenols were firstly O-carboxymethylated to prepare the corresponding p-substituted phenoxymethyl acids, which then reacted with o-phenylendiamine to get the key intermediates 2-(p-substituted) phenoxymethyl benzimidazole. Finally, the solid-liquid phase transfer catalysis method, where tetrabutyl ammonium bromide (TBAB) was used as the catalyst, was applied to synthesize the target compounds c/sub 1/-c/sub 5/ by the N-hydroxyethylation reaction with 2-chloroethyl alcohol. The structures of the obtained compounds were well characterized and confirmed by elemental analysis, MS, IR, /sup 1/H NMR, /sup 13/C NMR and single-crystal X-ray diffraction analysis. (author)

Effect of the physicochemical parameters of benzimidazole molecules on their retention by a nonpolar sorbent from an aqueous acetonitrile solution

Science.gov (United States)

Shafigulin, R. V.; Safonova, I. A.; Bulanova, A. V.

2015-09-01

The effect of the structure of benzimidazoles on their chromatographic retention on octadecyl silica gel from an aqueous acetonitrile eluent was studied. One- and many-parameter correlation equations were obtained by linear regression analysis, and their prognostic potential in determining the retention factors of benzimidazoles under study was analyzed.

Growth Inhibition of Sporomusa ovata by Incorporation of Benzimidazole Bases into Cobamides

Science.gov (United States)

Mok, Kenny C.

2013-01-01

Phenolyl cobamides are unique members of a class of cobalt-containing cofactors that includes vitamin B12 (cobalamin). Cobamide cofactors facilitate diverse reactions in prokaryotes and eukaryotes. Phenolyl cobamides are structurally and chemically distinct from the more commonly used benzimidazolyl cobamides such as cobalamin, as the lower axial ligand is a phenolic group rather than a benzimidazole. The functional significance of this difference is not well understood. Here we show that in the bacterium Sporomusa ovata, the only organism known to synthesize phenolyl cobamides, several cobamide-dependent acetogenic metabolisms have a requirement or preference for phenolyl cobamides. The addition of benzimidazoles to S. ovata cultures results in a decrease in growth rate when grown on methanol, 3,4-dimethoxybenzoate, H2 plus CO2, or betaine. Suppression of native p-cresolyl cobamide synthesis and production of benzimidazolyl cobamides occur upon the addition of benzimidazoles, indicating that benzimidazolyl cobamides are not functionally equivalent to the phenolyl cobamide cofactors produced by S. ovata. We further show that S. ovata is capable of incorporating other phenolic compounds into cobamides that function in methanol metabolism. These results demonstrate that S. ovata can incorporate a wide range of compounds as cobamide lower ligands, despite its preference for phenolyl cobamides in the metabolism of certain energy substrates. To our knowledge, S. ovata is unique among cobamide-dependent organisms in its preferential utilization of phenolyl cobamides. PMID:23417488

Uptake of benzimidazoles by Trichuris suis in vivo in pigs

DEFF Research Database (Denmark)

Hansen, Tina Vicky Alstrup; Friis, Christian; Nejsum, Peter

2014-01-01

It is recognized that the clinical efficacy of single dose benzimidazoles (BZs) against the nematode, Trichuris suis of pigs and the closely related Trichuris trichiura in humans is only poor to moderate. Recent in vitro studies have indicated that a low uptake of fenbendazole (FBZ) in T. suis may...

Slow, spontaneous degradation of lansoprazole, omeprazole and pantoprazole tablets: isolation and structural characterization of the toxic antioxidants 3H-benzimidazole-2-thiones.

Science.gov (United States)

Rajab, A; Touma, M; Rudler, H; Afonso, C; Seuleiman, M

2013-09-01

The spontaneous degradation of lansoprazole, omeprazole and pantoprazole tablets upon long-term and forced storage conditions was determined by high performance liquid chromatography (HPLC). The more abundant products could be isolated by liquid chromatography and their molecular weights determined by Mass Spectrometry (MS). Their structures, established according to their spectroscopic data, were compared to those of either the literature or of authentic samples. Thus lansoprazole led mainly to a mixture of 3H-benzimidazole-2-thione (2a) and 3H-benzimidazole-2-one (2c), omeprazole mainly to a mixture of 5-methoxy-3H-benzimidazole-2-thione (1a) and 2-hydroxymethyl-3, 5-dimethyl-4-methoxypyridine (1b), and pantoprazole, to 5-difluoromethoxy-3H-benzimidazole-2-thione (3a) and 2-hydroxymethyl-3, 4-dimethoxypyridine (3b). Although some of the degradation products had already been observed under different conditions, the detection of benzimidazole-2-thiones is unprecedented and their involvement as possible physiological, yet toxic antioxidants must be emphasized. Plausible, unified mechanisms for the formation of the different degradation products observed herein and in previous papers from the literature are suggested.

Saturn Rings Origin: Quantum Trapping of Superconducting Iced Particles and Meissner Effect Lead to the Stable Rings System

Science.gov (United States)

Viktorovich Tchernyi, Vladimir

2018-06-01

Saturn Rings Origin: Quantum Trapping of Superconducting Iced Particles and Meissner Effect Lead to the Stable Rings System Vladimir V. Tchernyi (Cherny), Andrew Yu. Pospelov Modern Science Institute, SAIBR, Moscow, Russia. E-mail: chernyv@bk.ruAbstractIt is demonstrated how superconducting iced particles of the protoplanetary cloud of Saturn are coming to magnetic equator plane and create the stable enough rings disk. There are two steps. First, after appearance of the Saturn magnetic field due to Meissner phenomenon all particles orbits are moving to the magnetic equator plane. Finally they become distributed as rings and gaps like iron particles around magnet on laboratory table. And they are separated from each other by the magnetic field expelled from them. It takes up to few tens of thousands years with ten meters rings disk thickness. Second, due to their quantum trapping all particles become to be trapped within magnetic well at the magnetic equator plane due to Abrikosov vortex for superconductor. It works even when particles have small fraction of superconductor. During the rings evolution some contribution to the disk also could come from the collision-generated debris of the current moon and from the geysers like it happened due to magnetic coupling of Saturn and Enceladus. The rings are relict of the early days of the magnetic field of Saturn system.

Activity of benzimidazoles against Dientamoeba fragilis (Trichomonadida, Monocercomonadidae) in vitro and correlation of beta-tubulin sequences as an indicator of resistance.

Science.gov (United States)

Stark, Damien; Barratt, Joel L N; Roberts, Tamalee; Marriott, Deborah; Harkness, John T; Ellis, John

2014-01-01

Recently, Dientamoeba fragilis has emerged as a significant and common enteropathogen. The majority of patients with dientamoebiasis present with gastrointestinal complaints and chronic symptoms are common. Numerous studies have successfully demonstrated parasite clearance, coupled with complete resolution of clinical symptoms following treatment with various antiparasitic compounds. Despite this, there is very little in vitro susceptibility data available for the organism. Benzimidazoles are a class of antiparasitic drugs that are commonly used for the treatment of protozoan and helminthic infections. Susceptibility testing was undertaken on four D. fragilis clinical isolates against the following benzimidazoles: albendazole, flubendazole, mebendazole, nocodazole, triclabendazole and thiabendazole. The activities of the antiprotozoal compounds at concentrations ranging from 2 μg/mL to 500 μg/mL were determined via cell counts of D. fragilis grown in xenic culture. All tested drugs showed no efficacy. The beta-tubulin transcript was sequenced from two of the D. fragilis isolates and amino acid sequences predicted a susceptibility to benzimidazoles. This is the first study to report susceptibility profiles for benzimidazoles against D. fragilis, all of which were not active against the organism. This study also found that beta-tubulin sequences cannot be used as a reliable marker for resistance of benzimidazoles in D. fragilis. D. Stark et al., published by EDP Sciences, 2014

Activity of benzimidazoles against Dientamoeba fragilis (Trichomonadida, Monocercomonadidae in vitro and correlation of beta-tubulin sequences as an indicator of resistance

Directory of Open Access Journals (Sweden)

Stark Damien

2014-01-01

Full Text Available Recently, Dientamoeba fragilis has emerged as a significant and common enteropathogen. The majority of patients with dientamoebiasis present with gastrointestinal complaints and chronic symptoms are common. Numerous studies have successfully demonstrated parasite clearance, coupled with complete resolution of clinical symptoms following treatment with various antiparasitic compounds. Despite this, there is very little in vitro susceptibility data available for the organism. Benzimidazoles are a class of antiparasitic drugs that are commonly used for the treatment of protozoan and helminthic infections. Susceptibility testing was undertaken on four D. fragilis clinical isolates against the following benzimidazoles: albendazole, flubendazole, mebendazole, nocodazole, triclabendazole and thiabendazole. The activities of the antiprotozoal compounds at concentrations ranging from 2 μg/mL to 500 μg/mL were determined via cell counts of D. fragilis grown in xenic culture. All tested drugs showed no efficacy. The beta-tubulin transcript was sequenced from two of the D. fragilis isolates and amino acid sequences predicted a susceptibility to benzimidazoles. This is the first study to report susceptibility profiles for benzimidazoles against D. fragilis, all of which were not active against the organism. This study also found that beta-tubulin sequences cannot be used as a reliable marker for resistance of benzimidazoles in D. fragilis.

Rings in drugs.

Science.gov (United States)

Taylor, Richard D; MacCoss, Malcolm; Lawson, Alastair D G

2014-07-24

We have analyzed the rings, ring systems, and frameworks in drugs listed in the FDA Orange Book to understand the frequency, timelines, molecular property space, and the application of these rings in different therapeutic areas and target classes. This analysis shows that there are only 351 ring systems and 1197 frameworks in drugs that came onto the market before 2013. Furthermore, on average six new ring systems enter drug space each year and approximately 28% of new drugs contain a new ring system. Moreover, it is very unusual for a drug to contain more than one new ring system and the majority of the most frequently used ring systems (83%) were first used in drugs developed prior to 1983. These observations give insight into the chemical novelty of drugs and potentially efficient ways to assess compound libraries and develop compounds from hit identification to lead optimization and beyond.

Complexes of molybdenum(III) with 2-(2'-pyridyl)benzimidazole

International Nuclear Information System (INIS)

Ghosh, S.P.; Prasad, K.M.

1979-01-01

Molybdenum(III) forms with 2-(2'-pyridyl) benzimidazole(LH) the trischelated complexes, [Mo(LH) 3 ]X 3 as well as the cationic-anionic complexes, [Mo(LH) 3 X 2 ] + [Mo(LH)X 4 ] - (X=Cl - ,Br - or NCS - ), depending on pH. These complexes have been synthesised and characterised from elemental analyses, i.r. and electronic spectra, magnetic moments and molar conductance. (auth.)

Voyager Saturnian ring measurements and the early history of the solar system

International Nuclear Information System (INIS)

Alfven, H.; Axnaes, I.; Brenning, N.; Lindqvist, P.A.

1986-01-01

The mass distribution in the Saturnian ring system is investigated and compared with predictions from the plasma cosmogony. According to this theory, the matter in the rings has once been in the form of a magnetized plasma, in which the gravitation is balanced partly by the centrifugal force and partly by the electromagnetic forces. As the plasma is neutralized, the electromagnetic forces disappear and the matter can be shown to fall in to 2/3 of the original saturnocentric distance. This causes the so called ''cosmogonic shadow effect'', which has been demonstrated earlier for the asteroidal belt and in the large scale structure of the Saturnian ring system. The relevance of the cosmogonic shadow effect is investigated for parts of the Saturnian ring system. It is shown that many structures of the present ring system can be understood as shadows and antishadows of cosmogonic origin. These appear in the form of double rings centered around a position a factor 0.64(slightly less than 2/3) closer to Saturn than the causing feature. Voyager data agree with an accuracy better than 1%. (author)

A ring transducer system for medical ultrasound research.

Science.gov (United States)

Waag, Robert C; Fedewa, Russell J

2006-10-01

An ultrasonic ring transducer system has been developed for experimental studies of scattering and imaging. The transducer consists of 2048 rectangular elements with a 2.5-MHz center frequency, a 67% -6 dB bandwidth, and a 0.23-mm pitch arranged in a 150-mm-diameter ring with a 25-mm elevation. At the center frequency, the element size is 0.30lambda x 42lambda and the pitch is 0.38lambda. The system has 128 parallel transmit channels, 16 parallel receive channels, a 2048:128 transmit multiplexer, a 2048:16 receive multiplexer, independently programmable transmit waveforms with 8-bit resolution, and receive amplifiers with time variable gain independently programmable over a 40-dB range. Receive signals are sampled at 20 MHz with 12-bit resolution. Arbitrary transmit and receive apertures can be synthesized. Calibration software minimizes system nonidealities caused by noncircularity of the ring and element-to-element response differences. Application software enables the system to be used by specification of high-level parameters in control files from which low-level hardware-dependent parameters are derived by specialized code. Use of the system is illustrated by producing focused and steered beams, synthesizing a spatially limited plane wave, measuring angular scattering, and forming b-scan images.

Spectral intensities and bonding parameters for some praseodymium(III) and neodymium(III) complexes with benzimidazoles

Energy Technology Data Exchange (ETDEWEB)

Vyas, P C; Ojha, C K; Mittal, S; Joshi, G K

1988-09-01

The electronic spectral intensity parameters (Judd-Ofelt; Tsub(lambda)) calculated from absorption spectral data for the complexes of praseodymium(III) and neodymium(III) nitrates with benzimidazole and 2-methyl-, 2-ethyl- and 2-n-propyl-benzimidazoles are reported. The conductance of these derivatives in dimethylformamide suggests 1:1 electrolytic nature. The infrared spectral data indicate the presence of Csub(2v) as well Dsub(2h)-nitrate ions in the complexes. The correlation of the intensity of hypersensitive transitions with bonding (nephelauxetic ratio and degree of covalency) parameters are also reported. (author). 13 refs., 2 tables.

In vitro activity of wALADin benzimidazoles against different life cycle stages of Plasmodium parasites.

Science.gov (United States)

Lentz, Christian S; Sattler, Julia M; Fendler, Martina; Gottwalt, Simon; Halls, Victoria S; Strassel, Silke; Arriens, Sandra; Hannam, Jeffrey S; Specht, Sabine; Famulok, Michael; Mueller, Ann-Kristin; Hoerauf, Achim; Pfarr, Kenneth M

2015-01-01

wALADin1 benzimidazoles are specific inhibitors of δ-aminolevulinic acid dehydratase from Wolbachia endobacteria of filarial nematodes. We report that wALADin1 and two derivatives killed blood stage Plasmodium falciparum in vitro (50% inhibitory concentrations, 39, 7.7, and 12.8 μM, respectively). One of these derivatives inhibited gliding motility of Plasmodium berghei ANKA infectious sporozoites with nanomolar affinity and blocked invasion into hepatocytes but did not affect intrahepatocytic replication. Hence, wALADin1 benzimidazoles are tools to study gliding motility and potential antiplasmodial drug candidates. Copyright © 2015, American Society for Microbiology. All Rights Reserved.

Synthesis of 1,2-Disubstituted Benzimidazoles in the Presence of SBA-Pr-SO3H as a Nano Solid Acid Catalyst

Directory of Open Access Journals (Sweden)

G. Mohammadi Ziarani

2012-06-01

Full Text Available In this article, simple, convenient synthesis of 2-aryl-1- arylmethyl-1H-1,3-benzimidazole (1,2-disubstituted benzimidazoles via condensation of 1,2-phenylenediamine and aromatic aldehydes using SBA-Pr-SO3H as a nanoporous solid acid catalyst in green protocol was reported.

Novel fluorinated benzimidazole-based scaffolds and their anticancer activity in vitro

Czech Academy of Sciences Publication Activity Database

Bhambra, A.S.; Edgar, M.; Elsegood, M.R.J.; Horsburgh, L.; Kryštof, Vladimír; Lucas, P.D.; Mojally, M.; Teat, S. J.; Warwick, T.G.; Weaver, G.W.; Zeinali, F.

2016-01-01

Roč. 188, AUG (2016), s. 99-109 ISSN 0022-1139 R&D Projects: GA ČR(CZ) GA15-15264S Institutional support: RVO:61389030 Keywords : Anticancer activity * Benzimidazole * C-F activation Subject RIV: FR - Pharmacology ; Medidal Chemistry Impact factor: 2.101, year: 2016

A progress report on the g-2 storage ring magnet system

International Nuclear Information System (INIS)

Bunce, G.; Cullen, J.; Danby, G.

1995-01-01

The 3.1 GeV muon storage ring for the g-2 experiment at Brookhaven National Laboratory hat three large solenoid magnets that form a continuous 1.451 tesla storage ring dipole with an average beam bond radius of 7.1 metors. In addition to the three storage ring solenoids, there is an inflector dipole with nested dipole coils that create very little stray magnetic field. A superconducting shield on the infractor gets rid of most of the remaining stray flux. This paper reports on the progress made on the storage ring solenoid magnet system and the inflector as of June 1995. The results of cryogenic system tests are briefly reported

Connections, curvature and cohomology

CERN Document Server

Greub, Werner H; Vanstone, Ray

1976-01-01

Imidazole and Benzimidazole Synthesis is a comprehensive survey of the known methods of syntheses and ring modification. It brings together the multitude of synthesis of the imidazole ring in a systemic way interms of specific bond formation, and recommends the most attractive synthetic approaches. It also collects non-ring-synthetic approaches to classes of compounds such as nitro-, halogeno-, and amino-imidazoles, and covers the synthesis of N-substituted compounds and preparations of specific isomers.

Beam position monitor system for storage rings

International Nuclear Information System (INIS)

Nakamura, M.; Hinkson, J.A.

1985-05-01

Beam position monitors (BPM) for synchrotron light storage rings usually consist of beam pickup electrodes, coaxial relays and a narrowband receiver. While accurate, these systems are slow and of limited use in the commissioning of an accelerator. A beam position monitor is described which is intended to be a principal diagnostic during debug and routine running of a storage ring. It is capable of measuring the position of a single bunch on the first or nth orbit to an accuracy of a few percent. Stored beam position is more accurately measured with averaging techniques. Beam position changes can be studied in a bandwidth from DC to a few MHz. The beam monitor electronics consist of a separate amplification, detection, and sampling channel for each beam pickup electrode. Fast switches in each channel permit selection of the nth turn for measurement (single bunch mode). A calibration pulse is injected into each channel after beam measurement to permit gain offsets to be measured and removed from the final data. While initially more costly than the usual beam position monitor system, this sytem will pay for itself in reduced storage ring debug and trouble shooting time. 5 refs., 5 figs

QSAR study of benzimidazole derivatives inhibition on escherichia coli methionine Aminopeptidase

Directory of Open Access Journals (Sweden)

Zahra Garkani-Nejad

2010-06-01

Full Text Available The paper describes a quantitative structure-activity relationship (QSAR study of IC50 values of benzimidazole derivatives on escherichia coli methionine aminopeptidase. The activity of the 32 inhibitors has been estimated by means of multiple linear regression (MLR and artificial neural network (ANN techniques. The results obtained using the MLR method indicate that the activity of derivatives of benzimidazoles on CoII-loaded escherichia coli methionine aminopeptidase depend on different parameters containing topological descriptors, Burden eigen values, 3D MoRSE descriptors and 2D autocorrelation descriptors. The best artificial neural network model is a fully-connected, feed forward back propagation network with a 5-4-1 architecture. Standard error for the training set using this network was 0.193 with correlation coefficient 0.996 and for the prediction set standard error was 1.41 with correlation coefficient 0.802. Comparison of the quality of the ANN with different MLR models showed that ANN has a better predictive power.

Single-pass BPM system of the Photon Factory storage ring.

Science.gov (United States)

Honda, T; Katoh, M; Mitsuhashi, T; Ueda, A; Tadano, M; Kobayashi, Y

1998-05-01

At the 2.5 GeV ring of the Photon Factory, a single-pass beam-position monitor (BPM) system is being prepared for the storage ring and the beam transport line. In the storage ring, the injected beam position during the first several turns can be measured with a single injection pulse. The BPM system has an adequate performance, useful for the commissioning of the new low-emittance lattice. Several stripline BPMs are being installed in the beam transport line. The continuous monitoring of the orbit in the beam transport line will be useful for the stabilization of the injection energy as well as the injection beam orbit.

Application of a Reverse Line Blot hybridisation assay for the species-specific identification of cyathostomins (Nematoda, Strongylida) from benzimidazole-treated horses in the Slovak Republic.

Science.gov (United States)

Cernanská, Dana; Paoletti, Barbara; Králová-Hromadová, Ivica; Iorio, Raffaella; Cudeková, Patrícia; Milillo, Piermarino; Traversa, Donato

2009-03-09

Five horse farms located in eastern Slovakia were investigated for the presence of benzimidazole-resistant strongyles by faecal egg count reduction test and egg hatch assay. Coprocultures were prepared for each farm from faecal samples taken pre- and post-treatment and harvested larvae were molecularly examined with a Reverse Line Blot assay. Faecal egg count reduction values ranged from 0 to 52.5% and all farms were positive for benzimidazole-resistant cyathostomins. Seven benzimidazole-resistant cyathostomin species were molecularly identified on farms before and also after treatment. These data demonstrate that resistance to benzimidazoles is well established in cyathostomin populations from horse farms in the Slovak Republic and that the molecular assay was able to determine the species-specific distribution of resistant cyathostomins under field conditions.

Real time global orbit feedback system for NSLS x-ray ring

International Nuclear Information System (INIS)

Yu, L.H.; Biscardi, R.; Bittner, J.; Fauchet, A.M.; Krinsky, F.S.; Nawrocky, R.J.; Rothman, J.; Singh, O.V.; Yang, K.M.

1991-01-01

We report on the design and commissioning of a real time harmonic global orbit feedback system for the NSLS X-ray ring. This system uses 8 pick-up electrode position monitors and 16 trim dipole magnets to eliminate 3 harmonic components of the orbit fluctuations. Because of the larger number of position monitors and trim magnets, the X-ray ring feedback system differs from the previously reported VUV ring system in that the Fourier analysis and harmonic generation networks are comprised of MDAC boards controlled by computer. The implementation of the global feedback system has resulted in a dramatic improvement of orbit stability, by more than a factor of five everywhere. Simultaneous operation of the global and several local bump feedback systems has been achieved. 4 refs., 5 figs

Radiation-induced conductivity of polynaphthoyl benzimidazole

Energy Technology Data Exchange (ETDEWEB)

Tiutnev, A P; Berlin, A M; Saenko, V S; Rusanov, A L; Korshak, V V

1985-01-01

The nonstationary radiation-induced conductivity of polynaphthoyl benzimidazole, synthesized by single-stage high-temperature catalytic polycondensation, is investigated experimentally. It is shown that the radiation-induced conductivity of this material is characterized by an anomalous (non-Gaussian) transfer of excess charge carriers. The activation energy of the delayed component (0.1 ms after pulse termination) is determined to be 0.12 eV; the volt-ampere characteristic of this component is nonlinear, with the coefficient of nonlinearity increasing with the intensity of the external electric field. Experimental results are interpreted on the basis of the phenomenological theory of jump conductivity proposed by Zviagin. 15 references.

Ring resonator systems to perform optical communication enhancement using soliton

CERN Document Server

Amiri, Iraj Sadegh

2014-01-01

The title explain new technique of secured and high capacity optical communication signals generation by using the micro and nano ring resonators. The pulses are known as soliton pulses which are more secured due to having the properties of chaotic and dark soliton signals with ultra short bandwidth. They have high capacity due to the fact that ring resonators are able to generate pulses in the form of solitons in multiples and train form. These pulses generated by ring resonators are suitable in optical communication due to use the compact and integrated rings system, easy to control, flexibi

A Bioinspired Catalytic Aerobic Oxidative C–H Functionalization of Primary Aliphatic Amines: Synthesis of 1,2-Disubstituted Benzimidazoles

Science.gov (United States)

Nguyen, Khac Minh Huy; Largeron, Martine

2015-01-01

Aerobic oxidative C–H functionalization of primary aliphatic amines has been accomplished with a biomimetic cooperative catalytic system to furnish 1,2-disubstituted benzimidazoles that play an important role as drug discovery targets. This one-pot atom-economical multistep process, which proceeds under mild conditions, with ambient air and equimolar amounts of each coupling partner, constitutes a convenient environmentally friendly strategy to functionalize non-activated aliphatic amines that remain challenging substrates for non-enzymatic catalytic aerobic systems. PMID:26206475

Transport of anthelmintic benzimidazole drugs by breast cancer resistance protein (BCRP/ABCG2)

NARCIS (Netherlands)

Merino, G; Jonker, JW; Wagenaar, E; Pulido, MM; Molina, AJ; Alvarez, AI; Schinkel, AH

Methylcarbamate benzimidazoles [albendazole (ABZ), fenbendazole (FBZ), and their respective sulfoxide derivatives, albendazole sulfoxide (ABZSO) and oxfendazole (OXF)] are therapeutically important anthelmintic agents with low bioavailability. We studied their in vitro interaction with the apical

Development of an Acoustic Levitation Linear Transportation System Based on a Ring-Type Structure.

Science.gov (United States)

Thomas, Gilles P L; Andrade, Marco A B; Adamowski, Julio Cezar; Silva, Emilio Carlos Nelli

2017-05-01

A linear acoustic levitation transportation system based on a ring-type vibrator is presented. The system is composed by two 21-kHz Langevin transducers connected to a ring-shaped structure formed by two semicircular sections and two flat plates. In this system, a flexural standing wave is generated along the ring structure, producing an acoustic standing wave between the vibrating ring and a plane reflector located at a distance of approximately a half wavelength from the ring. The acoustic standing wave in air has a series of pressure nodes, where small particles can be levitated and transported. The ring-type transportation system was designed and analyzed by using the finite element method. Additionally, a prototype was built and the acoustic levitation and transport of a small polystyrene particle was demonstrated.

Benzimidazole and its derivatives as corrosion inhibitors for mild steel in 1M HCl solution

International Nuclear Information System (INIS)

Aljourani, J.; Raeissi, K.; Golozar, M.A.

2009-01-01

In this paper, the inhibition ability of benzimidazole and its derivatives against the corrosion of mild steel in 1M HCl solution was studied. The change of impedance parameters observed by variation of inhibitors concentration within the range of 50-250 ppm was an indication of their adsorption. The thermodynamic adsorption parameters proposed that these inhibitors retard both cathodic and anodic processes through physical adsorption and blocking the active corrosion sites. The adsorption of these compounds obeyed the Langmuir's adsorption isotherm. The inhibition efficiency was increased with inhibitor concentration in the order of 2-mercaptobenzimidazole > 2-methylbenzimidazole > benzimidazole, which is in accordance with the variation of apparent activation energy of corrosion.

Fixation of carbon dioxide into dimethyl carbonate over titanium-based zeolitic thiophene-benzimidazolate framework

Data.gov (United States)

U.S. Environmental Protection Agency — A titanium-based zeolitic thiophene-benzimidazolate framework has been designed for the direct synthesis of dimethyl carbonate (DMC) from methanol and carbon...

Dragging of inertial frames in the composed black-hole-ring system

International Nuclear Information System (INIS)

Hod, Shahar

2015-01-01

A well-established phenomenon in general relativity is the dragging of inertial frames by a spinning object. In particular, due to the dragging of inertial frames by a ring orbiting a central black hole, the angular velocity Ω H BH-ring of the black-hole horizon in the composed black-hole-ring system is no longer related to the black-hole angular momentum J H by the simple Kerr-like (vacuum) relation Ω H Kerr (J H ) = J H /2M 2 R H (here M and R H are the mass and horizon-radius of the black hole, respectively). Will has performed a perturbative treatment of the composed black-hole-ring system in the regime of slowly rotating black holes and found the explicit relation Ω H BH-ring (J H = 0, J R , R) = 2J R /R 3 for the angular velocity of a central black hole with zero angular momentum, where J R and R are respectively the angular momentum of the orbiting ring and its proper circumferential radius. Analyzing a sequence of black-hole-ring configurations with adiabatically varying (decreasing) circumferential radii, we show that the expression found by Will for Ω H BH-ring (J H = 0, J R , R) implies a smooth transition of the central black-hole angular velocity from its asymptotic near-horizon value Ω H BH-ring (J H = 0, J R , R → R H + ) → 2J R /R H 3 (that is, just before the assimilation of the ring by the central black hole), to its final Kerr (vacuum) value Ω H Kerr (J H new )= J H new /2M new2 R H new [that is, after the adiabatic assimilation of the ring by the central black hole. Here J H new = J R , M new , and R H new are the new parameters of the resulting Kerr (vacuum) black hole after it assimilated the orbiting ring]. We use this important observation in order to generalize the result of Will to the regime of black-hole-ring configurations in which the central black holes possess non-zero angular momenta. In particular, it is shown that the continuity argument (namely, the characteristic smooth evolution of the black-hole angular velocity

Structure and magnetic field of periodic permanent magnetic focusing system with open magnetic rings

International Nuclear Information System (INIS)

Peng Long; Li Lezhong; Yang Dingyu; Zhu Xinghua; Li Yuanxun

2011-01-01

The magnetic field along the central axis for an axially magnetized permanent magnetic ring was investigated by analytical and finite element methods. For open magnetic rings, both calculated and measured results show that the existence of the radial magnetic field creates a remarkable cosine distribution field along the central axis. A new structure of periodic permanent magnet focusing system with open magnetic rings is proposed. The structure provides a satisfactory magnetic field with a stable peak value of 120 mT for a traveling wave tube system. - Research highlights: → For open magnetic rings, both calculated and measured results show that the existence of the radial magnetic field creates a remarkable cosine distribution field along the central axis. → A new structure of periodic permanent magnet (PPM) focusing system with open magnetic rings is proposed. → The new PPM focusing system with open magnetic rings meets the requirements for TWT system.

The vacuum interlock system for the CELSIUS ring

International Nuclear Information System (INIS)

Gajewski, K.

1990-01-01

A vacuum interlock system has been designed and built for the CELSIUS storage ring. The ultrahigh-vacuum system of CELSIUS has a design pressure of 10 -11 mbar. This is achieved by using vacuum-fired stainless-steel chambers, baking the whole ring to 300degC and running some 50 sputter ion and titanium sublimation pumps. The turbopumps, combined with roughing pumps, are used during the pump-down and the bake-out. The pressure is monitored by Penning vacuum gauges. There is a number of programmable pressure thresholds set to trigger various events (like closing the sector valves, disabling the bake-out, etc.). The interlock system is based on the Mitsubishi programmable logic controller (PLC). An IBM PC is used as an operator's console. The operation and performance of the system is described. On the basis of present experience an upgrading of the system is suggested. (orig.)

Coordination compounds of metals with imidazoles and benzimidazoles. [Metals: V, Th, Mo, Cd, rare earths, etc

Energy Technology Data Exchange (ETDEWEB)

Novikova, G A; Molodkin, A K; Kukalenko, S S

1988-12-01

Methods of preparation, composition and structure of UO/sub 2//sup 2+/, Th/sup 4+/, Mo/sup 3+/, Cd/sup 2+/, Ln/sup 3+/ metal ion complexes with imidazoles and benzimidazoles are considered in reviews of native and foreign literature of up to 1985. Complexes are customarily prepared by direct interaction of ligands with inorganic salts in different organic solvents. Complex composition is defined by the nature of complexing metal and inorganic salt anion, ligand volume and basicity, as well as solvent characteristics. Effect of R substituent in imidazole and benzimidazole side chain on composition of coordination compounds is considered.

Metabolic conversion of methyl benzimidazol 2 yl carbamate (MBC) in Aspergillus nidulans

NARCIS (Netherlands)

Davidse, L.C.

1976-01-01

Methyl benzimidazol 2 yl carbamate was metabolized by Aspergillus nidulans mycelium to two metabolites, one of which was identified as methyl 5 hydroxybenzimidazol 2 yl carbamate. This compound was further converted to a second metabolite which was not identified. Conversion rate was highest when

Above-room-temperature ferroelectricity and antiferroelectricity in benzimidazoles

Science.gov (United States)

Horiuchi, Sachio; Kagawa, Fumitaka; Hatahara, Kensuke; Kobayashi, Kensuke; Kumai, Reiji; Murakami, Youichi; Tokura, Yoshinori

2012-12-01

The imidazole unit is chemically stable and ubiquitous in biological systems; its proton donor and acceptor moieties easily bind molecules into a dipolar chain. Here we demonstrate that chains of these amphoteric molecules can often be bistable in electric polarity and electrically switchable, even in the crystalline state, through proton tautomerization. Polarization-electric field (P-E) hysteresis experiments reveal a high electric polarization ranging from 5 to 10 μC cm-2 at room temperature. Of these molecules, 2-methylbenzimidazole allows ferroelectric switching in two dimensions due to its pseudo-tetragonal crystal symmetry. The ferroelectricity is also thermally robust up to 400 K, as is that of 5,6-dichloro-2-methylbenzimidazole (up to ~373 K). In contrast, three other benzimidazoles exhibit double P-E hysteresis curves characteristic of antiferroelectricity. The diversity of imidazole substituents is likely to stimulate a systematic exploration of various structure-property relationships and domain engineering in the quest for lead- and rare-metal-free ferroelectric devices.

A Combination of 3D-QSAR, Molecular Docking and Molecular Dynamics Simulation Studies of Benzimidazole-Quinolinone Derivatives as iNOS Inhibitors

Directory of Open Access Journals (Sweden)

Peixun Liu

2012-09-01

Full Text Available Inducible Nitric Oxide Synthase (iNOS has been involved in a variety of diseases, and thus it is interesting to discover and optimize new iNOS inhibitors. In previous studies, a series of benzimidazole-quinolinone derivatives with high inhibitory activity against human iNOS were discovered. In this work, three-dimensional quantitative structure-activity relationships (3D-QSAR, molecular docking and molecular dynamics (MD simulation approaches were applied to investigate the functionalities of active molecular interaction between these active ligands and iNOS. A QSAR model with R2 of 0.9356, Q2 of 0.8373 and Pearson-R value of 0.9406 was constructed, which presents a good predictive ability in both internal and external validation. Furthermore, a combined analysis incorporating the obtained model and the MD results indicates: (1 compounds with the proper-size hydrophobic substituents at position 3 in ring-C (R3 substituent, hydrophilic substituents near the X6 of ring-D and hydrophilic or H-bond acceptor groups at position 2 in ring-B show enhanced biological activities; (2 Met368, Trp366, Gly365, Tyr367, Phe363, Pro344, Gln257, Val346, Asn364, Met349, Thr370, Glu371 and Tyr485 are key amino acids in the active pocket, and activities of iNOS inhibitors are consistent with their capability to alter the position of these important residues, especially Glu371 and Thr370. The results provide a set of useful guidelines for the rational design of novel iNOS inhibitors.

Model calibration and beam control systems for storage rings

International Nuclear Information System (INIS)

Corbett, W.J.; Lee, M.J.; Ziemann, V.

1993-04-01

Electron beam storage rings and linear accelerators are rapidly gaining worldwide popularity as scientific devices for the production of high-brightness synchrotron radiation. Today, everybody agrees that there is a premium on calibrating the storage ring model and determining errors in the machine as soon as possible after the beam is injected. In addition, the accurate optics model enables machine operators to predictably adjust key performance parameters, and allows reliable identification of new errors that occur during operation of the machine. Since the need for model calibration and beam control systems is common to all storage rings, software packages should be made that are portable between different machines. In this paper, we report on work directed toward achieving in-situ calibration of the optics model, detection of alignment errors, and orbit control techniques, with an emphasis on developing a portable system incorporating these tools

Complexes of molybdenum(III) with 2-(2'-pyridyl)benzimidazole

Energy Technology Data Exchange (ETDEWEB)

Ghosh, S P [Patna Univ. (India). Dept. of Chemistry; Prasad, K M [H.D. Jain Coll., Arrah (India). Dept. of Chemistry

1979-07-01

Molybdenum(III) forms with 2-(2'-pyridyl) benzimidazole(LH) the trischelated complexes, (Mo(LH)/sub 3/)X/sub 3/ as well as the cationic-anionic complexes, (Mo(LH)/sub 3/X/sub 2/)/sup +/ (Mo(LH)X/sub 4/)/sup -/(X=Cl/sup -/,Br/sup -/ or NCS/sup -/), depending on pH. These complexes have been synthesised and characterised from elemental analyses, i.r. and electronic spectra, magnetic moments and molar conductance.

The Abort Kicker System for the PEP-II Storage Rings at SLAC

International Nuclear Information System (INIS)

Delamare, Jeffrey E

2003-01-01

The PEP-II project has two storage rings. The HER (High Energy Ring) has up to 1.48 A of election beam at 9 GeV, and the LER (Low Energy Ring) has up to 2.14 A of positron beam at 3.1 GeV. To protect the HER and LER beam lines in the event of a ring component failure, each ring has an abort kicker system which directs the beam into a dump when a failure is detected. Due to the high current of the beams, the beam kick is tapered from 100% to 80% in 7.33 (micro)S (the beam transit time around the ring). This taper distributes the energy evenly across the window which separates the ring from the beam dump such that the window is not damaged. The abort kicker trigger is synchronized with the ion clearing gap of the beam allowing for the kicker field to rise from 0-80% while there is no beam in the kicker magnet. Originally the kicker system was designed for a rise time of 370nS [1], but because the ion clearing gap was reduced in half, so was the rise time requirement for the kicker. This report discusses the design of the system interlocks, diagnostics, and modulator with the modifications necessary to accommodate an ion clearing gap of 185nS

A Saturn Ring Observer Mission Using Multi-Mission Radioisotope Power Systems

International Nuclear Information System (INIS)

Abelson, Robert D.; Spilker, Thomas R.; Shirley, James H.

2006-01-01

Saturn remains one of the most fascinating planets within the solar system. To better understand the complex ring structure of this planet, a conceptual Saturn Ring Observer (SRO) mission is presented that would spend one year in close proximity to Saturn's A and B rings, and perform detailed observations and measurements of the ring particles and electric and magnetic fields. The primary objective of the mission would be to understand ring dynamics, including the microphysics of individual particles and small scale (meters to a few kilometers) phenomena such as particle agglomeration behavior. This would be accomplished by multispectral imaging of the rings at multiple key locations within the A and B rings, and by ring-particle imaging at an unprecedented resolution of 0.5 cm/pixel. The SRO spacecraft would use a Venus-Earth-Earth-Jupiter Gravity Assist (VEEJGA) and be aerocaptured into Saturn orbit using an advanced aeroshell design to minimize propellant mass. Once in orbit, the SRO would stand off from the ring plane 1 to 1.4 km using chemical thrusters to provide short propulsive maneuvers four times per revolution, effectively causing the SRO vehicle to 'hop' above the ring plane. The conceptual SRO spacecraft would be enabled by the use of a new generation of multi-mission Radioisotope Power Systems (RPSs) currently being developed by NASA and DOE. These RPSs include the Multi-Mission Radioisotope Thermoelectric Generator (MMRTG) and Stirling Radioisotope Generator (SRG). The RPSs would generate all necessary electrical power (≥330 We at beginning of life) during the 10-year cruise and 1-year science mission (∼11 years total). The RPS heat would be used to maintain the vehicle's operating and survival temperatures, minimizing the need for electrical heaters. Such a mission could potentially launch in the 2015-2020 timeframe, with operations at Saturn commencing in approximately 2030

Synthesis of substituted 2-(β-D-glucopyranosyl)-benzimidazoles and their evaluation as inhibitors of glycogen phosphorylase.

Science.gov (United States)

Bokor, Éva; Szilágyi, Enikő; Docsa, Tibor; Gergely, Pál; Somsák, László

2013-11-15

Microwave assisted condensation of O-perbenzoylated C-(β-d-glucopyranosyl)formic acid with 1,2-diaminobenzenes in the presence of triphenylphosphite gave the corresponding O-protected 2-(β-d-glucopyranosyl)-benzimidazoles in moderate yields. O-Perbenzoylated C-(β-d-glucopyranosyl)formamide and -thioformamide were transformed into the corresponding ethyl C-(β-d-glucopyranosyl)formimidate and -thioformimidate, respectively, by Et3O·BF4. Treatment of the formimidate with 1,2-diaminobenzenes afforded O-protected 2-(β-d-glucopyranosyl)-benzimidazoles in good to excellent yields. Similar reaction of the thioformimidate gave these compounds in lower yields. The O-benzoyl protecting groups were removed by the Zemplén protocol. These test compounds were assayed against rabbit muscle glycogen phosphorylase (GP) b, the prototype of liver GP, the rate limiting enzyme of glycogen degradation. The best inhibitors were 2-(β-d-glucopyranosyl)-4-methyl-benzimidazole (Ki=2.8μM) and 2-(β-d-glucopyranosyl)-naphtho[2,3-d]imidazole (Ki=2.1μM) exhibiting a ∼3-4 times stronger binding than the unsubstituted parent compound. Copyright © 2013 Elsevier Ltd. All rights reserved.

L-shaped benzimidazole fluorophores: synthesis, characterization and optical response to bases, acids and anions.

Science.gov (United States)

Lirag, Rio Carlo; Le, Ha T M; Miljanić, Ognjen Š

2013-05-14

Nine L-shaped benzimidazole fluorophores have been synthesized, computationally evaluated and spectroscopically characterized. These "half-cruciform" fluorophores respond to bases, acids and anions through changes in fluorescence that vary from moderate to dramatic.

Vortex rings in classical and quantum systems

International Nuclear Information System (INIS)

Barenghi, C F; Donnelly, R J

2009-01-01

The study of vortex rings has been pursued for decades and is a particularly difficult subject. However, the discovery of quantized vortex rings in superfluid helium has greatly increased interest in vortex rings with very thin cores. While rapid progress has been made in the simulation of quantized vortex rings, there has not been comparable progress in laboratory studies of vortex rings in a viscous fluid such as water. This article overviews the history and current frontiers of classical and quantum vortex rings. After introducing the classical results, this review discusses thin-cored vortex rings in superfluid helium in section 2, and recent progress in understanding vortex rings of very thin cores propagating in water in section 3. (invited paper)

Dynamical Evolution of Ring-Satellite Systems

Science.gov (United States)

Ohtsuki, Keiji

2005-01-01

The goal of this research was to understand dynamical processes related to the evolution of size distribution of particles in planetary rings and application of theoretical results to explain features in the present rings of giant planets. We studied velocity evolution and accretion rates of ring particles in the Roche zone. We developed a new numerical code for the evolution of ring particle size distribution, which takes into account the above results for particle velocity evolution and accretion rates. We also studied radial diffusion rate of ring particles due to inelastic collisions and gravitational encounters. Many of these results can be also applied to dynamical evolution of a planetesimal disk. Finally, we studied rotation rates of moonlets and particles in planetary rings, which would influence the accretional evolution of these bodies. We describe our key accomplishments during the past three years in more detail in the following.

Vanadium (4) complexing in phase of adsorbent with benzimidazole groups

International Nuclear Information System (INIS)

Shvoeva, O.P.; Kuchava, G.P.; Evtikova, G.A.; Belyaeva, V.K.; Myasoedova, G.V.; Marov, I.N.

1989-01-01

Equilibrium and kinetic characteristics of V 4+ sorption by POLYORGS XI-H adsorbent with benzimidazole groups (BIm) are investigated. Using ESR method it is stated that [VO 2+ ]:[BIm]1:2 complex, where VO 2+ is combined with nitrogen atoms of two imidazole groups, is formed in adsorbent phase. The highest distribution factor of 4.7x10 3 is attained at pH6

Dragging of inertial frames in the composed black-hole-ring system

Energy Technology Data Exchange (ETDEWEB)

Hod, Shahar [The Ruppin Academic Center, Emeq Hefer (Israel); The Hadassah Institute, Jerusalem (Israel)

2015-11-15

A well-established phenomenon in general relativity is the dragging of inertial frames by a spinning object. In particular, due to the dragging of inertial frames by a ring orbiting a central black hole, the angular velocity Ω{sub H}{sup BH-ring} of the black-hole horizon in the composed black-hole-ring system is no longer related to the black-hole angular momentum J{sub H} by the simple Kerr-like (vacuum) relation Ω{sub H}{sup Kerr}(J{sub H}) = J{sub H}/2M{sup 2}R{sub H} (here M and R{sub H} are the mass and horizon-radius of the black hole, respectively). Will has performed a perturbative treatment of the composed black-hole-ring system in the regime of slowly rotating black holes and found the explicit relation Ω{sub H}{sup BH-ring}(J{sub H} = 0, J{sub R}, R) = 2J{sub R}/R{sup 3} for the angular velocity of a central black hole with zero angular momentum, where J{sub R} and R are respectively the angular momentum of the orbiting ring and its proper circumferential radius. Analyzing a sequence of black-hole-ring configurations with adiabatically varying (decreasing) circumferential radii, we show that the expression found by Will for Ω{sub H}{sup BH-ring}(J{sub H} = 0, J{sub R}, R) implies a smooth transition of the central black-hole angular velocity from its asymptotic near-horizon value Ω{sub H}{sup BH-ring}(J{sub H} = 0, J{sub R}, R → R{sub H}{sup +}) → 2J{sub R}/R{sub H}{sup 3} (that is, just before the assimilation of the ring by the central black hole), to its final Kerr (vacuum) value Ω{sub H}{sup Kerr}(J{sub H}{sup new})= J{sub H}{sup new}/2M{sup new2}R{sub H}{sup new} [that is, after the adiabatic assimilation of the ring by the central black hole. Here J{sub H}{sup new} = J{sub R}, M{sup new}, and R{sub H}{sup new} are the new parameters of the resulting Kerr (vacuum) black hole after it assimilated the orbiting ring]. We use this important observation in order to generalize the result of Will to the regime of black-hole-ring configurations

Dragging of inertial frames in the composed black-hole–ring system

Energy Technology Data Exchange (ETDEWEB)

Hod, Shahar, E-mail: shaharhod@gmail.com [The Ruppin Academic Center, 40250, Emeq Hefer (Israel); The Hadassah Institute, 91010, Jerusalem (Israel)

2015-11-19

A well-established phenomenon in general relativity is the dragging of inertial frames by a spinning object. In particular, due to the dragging of inertial frames by a ring orbiting a central black hole, the angular velocity Ω{sub H}{sup BH-ring} of the black-hole horizon in the composed black-hole–ring system is no longer related to the black-hole angular momentum J{sub H} by the simple Kerr-like (vacuum) relation Ω{sub H}{sup Kerr}(J{sub H})=J{sub H}/2M{sup 2}R{sub H} (here M and R{sub H} are the mass and horizon-radius of the black hole, respectively). Will has performed a perturbative treatment of the composed black-hole–ring system in the regime of slowly rotating black holes and found the explicit relation Ω{sub H}{sup BH-ring}(J{sub H}=0,J{sub R},R)=2J{sub R}/R{sup 3} for the angular velocity of a central black hole with zero angular momentum, where J{sub R} and R are respectively the angular momentum of the orbiting ring and its proper circumferential radius. Analyzing a sequence of black-hole–ring configurations with adiabatically varying (decreasing) circumferential radii, we show that the expression found by Will for Ω{sub H}{sup BH-ring}(J{sub H}=0,J{sub R},R) implies a smooth transition of the central black-hole angular velocity from its asymptotic near-horizon value Ω{sub H}{sup BH-ring}(J{sub H}=0,J{sub R},R→R{sub H}{sup +})→2J{sub R}/R{sub H}{sup 3} (that is, just before the assimilation of the ring by the central black hole), to its final Kerr (vacuum) value Ω{sub H}{sup Kerr}(J{sub H}{sup new})=J{sub H}{sup new}/2M{sup new2}R{sub H}{sup new} [that is, after the adiabatic assimilation of the ring by the central black hole. Here J{sub H}{sup new}=J{sub R}, M{sup new}, and R{sub H}{sup new} are the new parameters of the resulting Kerr (vacuum) black hole after it assimilated the orbiting ring]. We use this important observation in order to generalize the result of Will to the regime of black-hole–ring configurations in which the

The synthesis of benzimidazoles and quinoxalines from aromatic diamines and alcohols by iridium-catalyzed acceptorless dehydrogenative alkylation.

Science.gov (United States)

Hille, Toni; Irrgang, Torsten; Kempe, Rhett

2014-05-05

Benzimidazoles and quinoxalines are important N-heteroaromatics with many applications in pharmaceutical and chemical industry. Here, the synthesis of both classes of compounds starting from aromatic diamines and alcohols (benzimidazoles) or diols (quinoxalines) is reported. The reactions proceed through acceptorless dehydrogenative condensation steps. Water and two equivalents of hydrogen are liberated in the course of the reactions. An Ir complex stabilized by the tridentate P^N^P ligand N(2) ,N(6) -bis(di-isopropylphosphino)pyridine-2,6-diamine revealed the highest catalytic activity for both reactions. © 2014 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

Synthesis and study of rhenium (5) complexes with benzimidazole and rubeanic acid

Energy Technology Data Exchange (ETDEWEB)

Basitova, S M; Yurina, R D; Kotegov, K V; Amindzhanov, A A

1986-01-01

Mixed rhenium (5) oxohalide complex compounds with benzimidazole and rubeanic acid are synthesized. Composition of the compounds obtained is established by IR spectroscpy thermal and chemical analyses. It is shown that rhenium (5) chloride compound stability to pyrolysis is rather lower than that of the corresponding bromide derivatives.

Synthesis and study of rhenium (5) complexes with benzimidazole and rubeanic acid

International Nuclear Information System (INIS)

Basitova, S.M.; Yurina, R.D.; Kotegov, K.V.; Amindzhanov, A.A.

1986-01-01

Mixed rhenium (5) oxohalide complex compounds with benzimidazole and rubeanic acid are synthesized. Composition of the compounds obtained is established by IR spectroscpy thermal and chemical analyses. It is shown that rhenium (5) chloride compound stability to pyrolysis is rather lower than that of the corresponding bromide derivatives

A pilot investigation to constrain the presence of ring systems around transiting exoplanets

Science.gov (United States)

Hatchett, W. Timothy; Barnes, Jason W.; Ahlers, John P.; MacKenzie, Shannon M.; Hedman, Matthew M.

2018-04-01

We demonstrate a process by which to evaluate the presence of large, Saturn-like ring systems around transiting extrasolar giant planets. We use extrasolar planet candidate KOI-422.01 as an example around which to establish limits on the presence of ring systems. We find that the spherical-planet (no-rings) fit matches the lightcurve of KOI-422.01 better than a lightcurve with a planet having obliquity angles 90°, 60°, 45°, or 20°. Hence we find no evidence for rings around KOI-422.01, but the methods that we have developed can be used for more comprehensive ring searches in the future. If the Hedman (2015) low-temperature rings hypothesis is correct, then the first positive detection of exorings might require transits of very long period ( ≳ 10 yr) giant planets outside their stars' ice lines.

Efficient fluorescent deep-blue and hybrid white emitting devices based on carbazole/benzimidazole compound

KAUST Repository

Yang, Xiaohui; Zheng, Shijun; Bottger, Rebecca; Chae, HyunSik; Tanaka, Takeshi; Li, Sheng; Mochizuki, Amane; Jabbour, Ghassan E.

2011-01-01

We report the synthesis, photophysics, and electrochemical characterization of carbazole/benzimidazole-based compound (Cz-2pbb) and efficient fluorescent deep-blue light emitting devices based on Cz-2pbb with the peak external quantum efficiency

Synthesis of Benzimidazole Derivatives: As Anti-hypertensive Agents

Directory of Open Access Journals (Sweden)

Jat Rakesh Kumar

2006-01-01

Full Text Available A new series of non peptide angiotensin(A-II receptor antagonist has been prepared. This N-(biphenyl methyl imidazoles e.g. 5-substituted (amino -2- phenyl-1-(2ʼcarboxy biphenyl-4-yl benzimidazoles differ from the previously reported and related compounds in that they produce a potent hypertensive effect upon oral administration. The earlier series were generally active only when administered intravenously. It has been found that 2’-position of biphenyl is essential. Only ortho substituted acid possess both high affinity for the AII receptor and oral anti-hypertensive potency.

Numerical simulation study on new RF system of Hefei storage ring

International Nuclear Information System (INIS)

Xu Hongliang; Wang Lin; Huang Guirong; Zhang Pengfei; Li Weimin; Liu Zuping; He Duohui

2005-01-01

The two injection ways of new RF system of Hefei storage ring were discussed. In the process of both large detuning injection and tuning injection, the variation of tuning angle and visual detuning angle with beam current intensity was analyzed. The calculation results show that the two injection ways are manipulable for new RF system in phase II project of Hefei storage ring. (author)

A fluorescence switch based on a controllable photochromic naphthopyran group

International Nuclear Information System (INIS)

Chen Lizhen; Wang Guang; Zhao Xiancai

2011-01-01

A fluorescence switch based on photoisomerization of naphthopyran (NP) has been designed by employing 2-(pyridin-2-yl)-benzimidazole (BPI) and the naphthopyran containing two pyran rings (NP) as fluorescent dye and photochromic compound, respectively. The fluorescence switch of benzimidazole derivative can be modulated either by controlling the irradiation time of UV light or by adjusting the amount ratio of fluorescent benzimidazole derivative to photochromic naphthopyran in both solution and polymethyl methacrylate (PMMA) film. The experimental results indicated that the decrease of fluorescence intensity of benzimidazole derivative is attributed to the interaction of benzimidazole with naphthopyran. - Highlights: → Naphthopyran was first used to fabricate fluorescence switch with benzimidazole derivative. → Fluorescence intensity can be modulated by controlling the UV irradiation time. → Fluorescence intensity can be adjusted by changing the ratio of benzimidazole derivative to naphthopyran. → Decrease of fluorescence intensity is attributed to the interaction of benzimidazole derivative and naphthopyran.

Proton storage ring (PSR) diagnostics and control system

International Nuclear Information System (INIS)

Clout, P.

1983-01-01

When any new accelerator or storage ring is built that advances the state of the art, the diagnostic system becomes extremely important in tuning the facility to full specification. This paper will discuss the various diagnostic devices planned or under construction for the PSR and their connection into the control system

Design for ANL 7 GeV storage ring vacuum system

International Nuclear Information System (INIS)

Wehrle, R.B.; Nielsen, R.W.

1988-01-01

The 7-GeV Advanced Photon Source (APS) design includes a storage ring having a 1060-m circumference with the capability of accommodating 34 insertion devices (ID) and their associated photon beam lines. An additional 35 photon lines can be provided from bending magnets. The vacuum system for the storage ring is designed to maintain a beam-on operating pressure of 1n Torr or less to achieve a positron beam lifetime of approximately 20 hours. The vacuum system and it's current developmental status are described

Vanadium (4) complexing in phase of adsorbent with benzimidazole groups

Energy Technology Data Exchange (ETDEWEB)

Shvoeva, O P; Kuchava, G P; Evtikova, G A; Belyaeva, V K; Myasoedova, G V; Marov, I N [AN SSSR, Moscow (USSR). Inst. Geokhimii i Analiticheskoj Khimii

1989-04-01

Equilibrium and kinetic characteristics of V{sup 4+} sorption by POLYORGS XI-H adsorbent with benzimidazole groups (BIm) are investigated. Using ESR method it is stated that (VO{sup 2+}):(BIm)1:2 complex, where VO{sup 2+} is combined with nitrogen atoms of two imidazole groups, is formed in adsorbent phase. The highest distribution factor of 4.7x10{sup 3} is attained at pH6.

The Abort Kicker System for the PEP-II Storage Rings at SLAC.

CERN Document Server

Delamare, J E

2003-01-01

The PEP-II project has two storage rings. The HER (High Energy Ring) has up to 1.48 A of election beam at 9 GeV, and the LER (Low Energy Ring) has up to 2.14 A of positron beam at 3.1 GeV. To protect the HER and LER beam lines in the event of a ring component failure, each ring has an abort kicker system which directs the beam into a dump when a failure is detected. Due to the high current of the beams, the beam kick is tapered from 100% to 80% in 7.33 (micro)S (the beam transit time around the ring). This taper distributes the energy evenly across the window which separates the ring from the beam dump such that the window is not damaged. The abort kicker trigger is synchronized with the ion clearing gap of the beam allowing for the kicker field to rise from 0-80% while there is no beam in the kicker magnet. Originally the kicker system was designed for a rise time of 370nS [1], but because the ion clearing gap was reduced in half, so was the rise time requirement for the kicker. This report discusses the des...

The discussion of descriptors for the QSAR model and molecular dynamics simulation of benzimidazole derivatives as corrosion inhibitors

International Nuclear Information System (INIS)

Li, Lu; Zhang, Xiuhui; Gong, Shida; Zhao, Hongxia; Bai, Yang; Li, Qianshu; Ji, Lin

2015-01-01

Graphical abstract: - Highlights: • Aromaticity is used as a descriptor in QSAR model to describe corrosion inhibition. • Improved calculation of I and A is correlated well with inhibition efficiencies. • Binding energies were calculated using a realistic corrosion environment. • Nonlinear QSAR model was built by support vector machine with radial basis function. • Six designed benzimidazole molecules are predicted with high inhibition efficiencies. - Abstract: The corrosion inhibition performances of 20 protonated benzimidazole derivatives were studied using theoretical methods. Nuclear Independent Chemical Shift (NICS), the measurement of aromaticity, demonstrated good correlation with inhibition efficiencies and was used as a descriptor. Binding energies were calculated on the basis of molecular dynamics simulations using a realistic corrosive environment. Some improved descriptors correlate well with experimental inhibition efficiencies. A reliable nonlinear quantitative structure–activity relationship model was constructed by a support vector machine approach. The correlation coefficient and root-mean-square error were 0.96 and 6.79%, respectively. Additionally, six new benzimidazole molecules were designed, and their inhibition efficiencies were predicted.

The g-2 storage ring superconducting magnet system

International Nuclear Information System (INIS)

Green, M.A.

1993-09-01

The g-2 μ lepton (muon) storage ring is a single dipole magnet that is 44 meters in circumference. The storage ring dipole field is created by three large superconducting solenoid coils. A single outer solenoid, 15.1 meters in diameter, carries 254 kA. Two inner solenoids, 13.4 meters in diameter, carry 127 kA each in opposition to the current carried by the outer solenoid. A room temperature C shaped iron yoke returns the magnetic flux and shapes the magnetic field in a 180 mm gap where the stored muon beam circulates. The gap induction will be 1.47 T. This report describes the three large superconducting solenoids, the cryogenic system needed to keep them cold, the solenoid power supply and the magnet quench protection system

3,4-Dimethoxyphenyl bis-benzimidazole, a novel DNA topoisomerase inhibitor that preferentially targets Escherichia coli topoisomerase I

Science.gov (United States)

Bansal, Sandhya; Sinha, Devapriya; Singh, Manish; Cheng, Bokun; Tse-Dinh, Yuk-Ching; Tandon, Vibha

2012-01-01

Objectives Antibiotic resistance in bacterial pathogens is a serious clinical problem. Novel targets are needed to combat increasing drug resistance in Escherichia coli. Our objective is to demonstrate that 2-(3,4-dimethoxyphenyl)-5-[5-(4-methylpiperazin-1-yl)-1H-benzimidazol-2yl]-1H-benzimidazole (DMA) inhibits E. coli DNA topoisomerase I more strongly than human topoisomerase I. In addition, DMA is non-toxic to mammalian cells at antibiotic dosage level. Methods In the present study, we have established DMA as an antibacterial compound by determining MICs, post-antibiotic effects (PAEs) and MBCs for different standard as well as clinical strains of E. coli. We have described the differential catalytic inhibitory mechanism of bis-benzimidazole, DMA, for human and E. coli topoisomerase I and topoisomerase II by performing different assays, including relaxation assays, cleavage–religation assays, DNA unwinding assays, ethidium bromide displacement assays, decatenation assays and DNA gyrase supercoiling assays. Results DMA significantly inhibited bacterial growth at a very low concentration, but did not affect human cell viability at higher concentrations. Activity assays showed that it preferentially targeted E. coli topoisomerase I over human topoisomerase I, topoisomerase II and gyrase. Cleavage–religation assays confirmed DMA as a poison inhibitor of E. coli topoisomerase I. This study illuminates new properties of DMA, which may be further modified to develop an efficient topoisomerase inhibitor that is selective towards bacterial topoisomerase I. Conclusions This is the first report of a bis-benzimidazole acting as an E. coli topoisomerase I inhibitor. DMA is a safe, non-cytotoxic molecule to human cells at concentrations that are needed for antibacterial activity. PMID:22945915

Metal-containing Complexes of Lactams, Imidazoles, and Benzimidazoles and Their Biological Activity

Science.gov (United States)

Kukalenko, S. S.; Bovykin, B. A.; Shestakova, S. I.; Omel'chenko, A. M.

1985-07-01

The results of the latest investigations of the problem of the synthesis of metal-containing complexes of lactams, imidazoles, and benzimidazoles, their structure, and their stability in solutions are surveyed. Some data on their biological activity (pesticide and pharmacological) and the mechanism of their physiological action are presented. The bibliography includes 190 references.

Storage Rings

International Nuclear Information System (INIS)

Fischer, W.

2010-01-01

Storage rings are circular machines that store particle beams at a constant energy. Beams are stored in rings without acceleration for a number of reasons (Tab. 1). Storage rings are used in high-energy, nuclear, atomic, and molecular physics, as well as for experiments in chemistry, material and life sciences. Parameters for storage rings such as particle species, energy, beam intensity, beam size, and store time vary widely depending on the application. The beam must be injected into a storage ring but may not be extracted (Fig. 1). Accelerator rings such as synchrotrons are used as storage rings before and after acceleration. Particles stored in rings include electrons and positrons; muons; protons and anti-protons; neutrons; light and heavy, positive and negative, atomic ions of various charge states; molecular and cluster ions, and neutral polar molecules. Spin polarized beams of electrons, positrons, and protons were stored. The kinetic energy of the stored particles ranges from 10 -6 eV to 3.5 x 10 12 eV (LHC, 7 x 10 12 eV planned), the number of stored particles from one (ESR) to 1015 (ISR). To store beam in rings requires bending (dipoles) and transverse focusing (quadrupoles). Higher order multipoles are used to correct chromatic aberrations, to suppress instabilities, and to compensate for nonlinear field errors of dipoles and quadrupoles. Magnetic multipole functions can be combined in magnets. Beams are stored bunched with radio frequency systems, and unbunched. The magnetic lattice and radio frequency system are designed to ensure the stability of transverse and longitudinal motion. New technologies allow for better storage rings. With strong focusing the beam pipe dimensions became much smaller than previously possible. For a given circumference superconducting magnets make higher energies possible, and superconducting radio frequency systems allow for efficient replenishment of synchrotron radiation losses of large current electron or positron beams

Metal-free TEMPO-promoted C(sp³)-H amination to afford multisubstituted benzimidazoles.

Science.gov (United States)

Xue, Ding; Long, Ya-Qiu

2014-05-16

An efficient TEMPO-air/cat. TEMPO-O2 oxidative protocol was developed to synthesize multisubstituted or fused tetracyclic benzimidazoles via a metal-free oxidative C-N coupling between the sp(3) C-H and free N-H of readily available N(1)-benzyl/alkyl-1,2-phenylenediamines.

Complexes cobalt(II, zinc(II and copper(II with some newly synthesized benzimidazole derivatives and their antibacterial activity

Directory of Open Access Journals (Sweden)

S. O. PODUNAVAC-KUZMANOVIC

1999-05-01

Full Text Available The preparation and properties of some complexes of cobalt(II, zinc(II and copper(II with several newly synthesized benzimidazole derivatives (L are reported. The complexes, of the general formula [MCl2L2] (M=Co(II, Zn(II and [CuCl2L(H2O], have a tetrahedral structure. The complexes were characterized by elemental analysis, molar conductivity, magnetic susceptibility measurements, IR and absorption electronic spectra. The antibacterial activitiy of the benzimidazoles and their complexes was evaluated against Erwinia carotovora subsp. carotovora and Erwinia amylovora. The complexes were found to be more toxic than the ligands.

Silane Cross-Linked Sulfonted Poly(Ether Ketone/Ether Benzimidazoles for Fuel Cell Applications

Directory of Open Access Journals (Sweden)

Zilu Yao

2017-11-01

Full Text Available γ-(2,3-epoxypropoxy propyltrimethoxysilane (KH-560 was incorporated in various proportions into side-chain-type sulfonated poly(ether ketone/ether benzimidazole (SPEKEBI as a crosslinker, to make membranes with high ion exchange capacities and excellent performance for direct methanol fuel cells (DMFCs. Systematical measurements including Fourier transform infrared (FT-IR, scanning electron microscopy-energy-dispersive and X-ray photoelectron spectroscopy (XPS proved the complete disappearance of epoxy groups in KH-560 and the existence of Si in the membranes. The resulting membranes showed increased mechanical strength and thermal stability compared to the unmodified sulfonated poly(ether ketone/ether benzimidazole membrane in appropriate doping amount. Meanwhile, the methanol permeability has decreased, leading to the increase of relative selectivities of SPEKEBI-x-SiO2 membranes. Furthermore, the H2/O2 cell performance of SPEKEBI-2.5-SiO2 membrane showed a much higher peak power density compared with the pure SPEKEBI memrbrane.

The Age of Saturn's Rings Constrained by the Meteoroid Flux Into the System

Science.gov (United States)

Kempf, S.; Altobelli, N.; Srama, R.; Cuzzi, J. N.; Estrada, P. R.

2017-12-01

The origin of Saturn's ring is still not known. There is an ongoing argument whether Saturn's ring are rather young or have been formed shortly after Saturn together with its satellites. The water-ice rings contain about 5% rocky material resulting from continuous meteoroid bombardment of the ring material with interplanetary micrometeoroids. Knowledge of the incoming mass flux would allow to estimate the ring's exposure time. Model calculations suggest exposure times of 108 years implying a late ring formation. This scenario is problematic because the tidal disruption of a Mimas-sized moon or of a comet within the planet's Roche zone would lead to a much larger rock content as observed today. Here we report on the measurement of the meteoroid mass flux into the Saturnian system obtained by the charge-sensitive entrance grid system (QP) of the Cosmic Dust Analyser (CDA) on the Cassini spacecraft. Interplanetary dust particles (IDPs) entering Saturn's sphere of gravitational influence are identified through the measurements of their speed vectors. We analyzed the full CDA data set acquired after Cassini's arrival at Saturn in 2004, identified the impact speed vectors of 128 extrinsic micrometeoroids ≥ 2 μm, and determined their orbital elements. On the basis of these measurements we determined the mass flux into the Saturnian system. Our preliminary findings are in support of an old ring. The knowledge of the meteoroids orbital elements allows us for the first time to characterize the meteoroid environment in the outer solar system based on direct measurements.

An application of ultrasonic inspection system (INER-SCAN) inspecting generator retaining rings

International Nuclear Information System (INIS)

Chen, L.C.; Hwang, S.C.

1994-01-01

The performances of the automatic ultrasonic inspecting and imaging system (INER-SCAN) developed by the NDT laboratory of the Institute of Nuclear Energy Research have been enhanced and much more improved to commercial level. With appropriate rearrangements of software libraries, it is used to inspect generator retaining rings which are critical structural rotor components that support the end-turn regions of the rotor wingings against centrifugal forces. The use of the INER-SCAN provides distinct advantages over other systems in terms of the reliability of inspection and the flexibility of system performance modifications. The INER-SCAN system assists users to select and modify ultrasonic parameters under computer-aided environment. In addition, the INER-SCAN system contains the necessary software functions to image the ultrasonic data (A-SCAN, B-SCAN, B'-SCAN, C-SCAN). The use of the imaging system makes it quite easy to evaluate various test parameters and their effects on the discrimination between geometric and IGSCC reflectors. Through experimental test, it is recognized that the system has powerful detectable capability which can find 0.2mm-depth slight scratch on the inner surface of retaining rings. This system can also be used on different generator retaining rings (different in terms of hidden design features) without the need for access to the dimension of retaining ring

Beam vacuum system of Brookhaven's muon storage ring

International Nuclear Information System (INIS)

Hseuth, H.C.; Snydstrup, L.; Mapes, M.

1995-01-01

A storage ring with a circumference of 45 m is being built at Brookhaven to measure the g-2 value of the muons to an accuracy of 0.35 ppm.. The beam vacuum system of the storage ring will operate at 10 -7 Torr and has to be completely non-magnetic. It consists of twelve sector chambers. The chambers are constructed of aluminum and are approximately 3.5 m in length with a rectangular cross-section of 16.5 cm high by 45 cm at the widest point. The design features, fabrication techniques and cleaning methods for these chambers are described. The beam vacuum system will be pumped by forty eight non-magnetic distributed ion pumps with a total pumping speed of over 2000 ell/sec. Monte Carlo simulations of the pressure distribution in the muon storage region are presented

Activity of cationically substituted bis-benzimidazoles against experimental Pneumocystis carinii pneumonia.

Science.gov (United States)

Tidwell, R R; Jones, S K; Naiman, N A; Berger, L C; Brake, W B; Dykstra, C C; Hall, J E

1993-01-01

On the basis of a previously observed correlation between the antimicrobial activity and DNA binding strength of dicationic molecules, a series of 10 dicationically substituted bis-benzimidazoles were tested for activity in the rat model of Pneumocystis carinii pneumonia. One of the compounds, 1,4-bis[5-(2-imidazolinyl)-2-benzimidazolyl]butane, was found to be more potent and less toxic than pentamidine. PMID:8215291

Mild and Efficient One Pot Synthesis of Imidazolinesand Benzimidazoles from Aldehydes

Directory of Open Access Journals (Sweden)

Rajesh Kumar

2007-01-01

Full Text Available A series of some imidazolines and benzimidazoles were synthesizedfrom various aldehydes and 1,2-diamines in the presence of ceric(IVammonium nitrate (CAN. The title compounds were prepared via one stepsynthesis method. The simplicity of the reaction conditions with shorterreaction time and with out use of column chromatography to get the pureproducts in high yields makes this method more attractive for organic chemists.

Convergent synthesis of the HIJKLM ring system of ciguatoxin CTX3C.

Science.gov (United States)

Takamura, Hiroyoshi; Nishiuma, Naoki; Abe, Takashi; Kadota, Isao

2011-09-02

The HIJKLM ring system of ciguatoxin CTX3C was synthesized in a convergent manner. The key steps were a conjugate addition/alkylation sequence, spiroacetalization, intramolecular allylation, ring-closing metathesis, and hydrogenation to form the 36-α-methyl substituent.

Laser action benzimidazoles in various aggregate states

Science.gov (United States)

Gruzinskii, V. V.; Degtiarenko, K. M.; Shalaev, V. K.; Kopylova, T. N.; Verkhovskii, V. S.; Tarasenko, V. F.; Melchenko, S. V.

1983-04-01

Lasing has been obtained in solutions of benzimidazole (Bi) derivatives: 2-phenyl-Bi (with the band maximum lambda-r-max = 341-347 nm), 2-n-tolyl-Bi (344 nm), and 2-(4'-biphenilyl) Bi (366-374 nm). It is found that compounds of this class provide a basis for laser radiation covering a wide region of the spectrum. Lasing has been obtained on the vapors of 2-(4'-biphenilyl) Bi (361.2 nm) and 2-(n-tolyl) Bi (336.5 nm) with a pentane stabilizer of the excited states. High volatility, photostability, and lasing in wide ranges of concentration determine the efficiency of using this new class of compounds (chain arylbenzimidazoles) in lasers using the vapors of complex molecules.

Laser action benzimidazoles in various aggregate states

Energy Technology Data Exchange (ETDEWEB)

Gruzinskii, V V; Degtiarenko, K M; Shalaev, V K; Kopylova, T N; Verkhovskii, V S; Tarasenko, V F; Melchenko, S V

1983-04-01

Lasing has been obtained in solutions of benzimidazole (Bi) derivatives: 2-phenyl-Bi (with the band maximum lambda-r-max 341-347 nm), 2-n-tolyl-Bi (344 nm), and 2-(4'-biphenilyl) Bi (366-374 nm). It is found that compounds of this class provide a basis for laser radiation covering a wide region of the spectrum. Lasing has been obtained on the vapors of 2-(4'-biphenilyl) Bi (361.2 nm) and 2-(n-tolyl) Bi (336.5 nm) with a pentane stabilizer of the excited states. High volatility, photostability, and lasing in wide ranges of concentration determine the efficiency of using this new class of compounds (chain arylbenzimidazoles) in lasers using the vapors of complex molecules.

RF SYSTEM FOR THE SNS ACCUMULATOR RING

International Nuclear Information System (INIS)

BLASKIEWICZ, M.; BRENNAN, J.M.; BRODOWSKI, J.; DELONG, J.; METH, M.; SMITH, K.; ZALTSMAN, A.

2001-01-01

During accumulation the RF beam current in the spallation neutron source ring rises from 0 to 50 amperes. A clean, 250 nanosecond gap is needed for the extraction kicker risetime. Large momentum spread and small peak current are needed to prevent instabilities and stopband related losses. A robust RF system meeting these requirements has been designed

A concise synthesis of benzimidazoles via the microwave-assisted one-pot batch reaction of amino acids up to a 10-g scale.

Science.gov (United States)

Peng, Pai; Xiong, Jin-Feng; Mo, Guang-Zhen; Zheng, Jia-Li; Chen, Ren-Hong; Chen, Xiao-Yun; Wang, Zhao-Yang

2014-10-01

An efficient method for the synthesis of aminomethyl benzimidazoles is developed by using a one-pot batch reaction between amino acids and o-phenylenediamines. This reaction proceeds smoothly in an unmodified household microwave oven, even though scale-up is to 10 g. A desirable method for the quick synthesis of benzimidazoles, which are used as a kind of important intermediates in drug synthesis, is provided by the scale-up utilization of amino acid resource.

Ring interconnection for distributed memory automation and computing system

Energy Technology Data Exchange (ETDEWEB)

Vinogradov, V I [Inst. for Nuclear Research of the Russian Academy of Sciences, Moscow (Russian Federation)

1996-12-31

Problems of development of measurement, acquisition and central systems based on a distributed memory and a ring interface are discussed. It has been found that the RAM LINK-type protocol can be used for ringlet links in non-symmetrical distributed memory architecture multiprocessor system interaction. 5 refs.

Oxovanadium(IV) complexes with tridentate dibasic schiff base ligands and 2-(2'-pyridyl) benzimidazole

Energy Technology Data Exchange (ETDEWEB)

Mohanty, R N; Chakravortty, V; Dash, K C [Utkal Univ., Bhubaneswar (India). Dept. of Chemistry

1991-05-01

The present work deals with the monomeric, six-coordinated mixed-ligand complexes of oxovanadium(IV) with dibasic tridentate schiff base ligands(ONO donor set) and the bidentate chelating ligand 2-(2'-pyridyl)benzimidazole (PBH) containing N{sub 2} donor set. (author). 1 tab., 22 refs.

Anion exchange membrane based on alkali doped poly(2,5-benzimidazole) for fuel cell

CSIR Research Space (South Africa)

Luo, H

2012-02-01

Full Text Available The properties of alkali doped poly(2,5-benzimidazole) membrane with different alkali doping level for fuel cell application is reported in this work. The alkali doping level played an important role for the ion conductivity of the membrane. The ion...

Alternative energy production pathways in Taenia crassiceps cysticerci in vitro exposed to a benzimidazole derivative (RCB20).

Science.gov (United States)

Fraga, Carolina Miguel; Da Costa, Tatiane Luiza; De Castro, Ana Maria; Reynoso-Ducoing, Olivia; Ambrosio, Javier; Hernández-Campos, Alicia; Castillo, Rafael; Vinaud, Marina Clare

2016-04-01

Biochemical studies of benzimidazole derivatives are important to determine their mode of action and activity against parasites. The lack of antihelminthic alternatives to treat parasitic infections and albendazole resistance cases make the search for new antiparasitary drugs of utmost importance. The 6-chloro-5-(1-naphthyloxy)-2-(trifluoromethyl)-1H-benzimidazole (RCB20) is a benzimidazole derivative with promising effect. This study evaluated the effect of different concentrations of RCB20 in the alternative energetic pathway of in vitro Taenia crassiceps cysticerci. The parasites were in vitro exposed to 6.5 and 13 µM of RCB20 and albendazole sulfoxide (ABZSO). The quantification of acetate, acetoacetate, β-hydroxybutyrate, fumarate and propionate was performed by high-performance liquid chromatography. The quantification of urea, creatinine and total proteins was performed by spectrophotometry. The increase in β-hydroxybutyrate reflects the enhancement of the fatty acid oxidation in the treated groups. Volatile fatty acids secretion, acetate and propionate, was increased in the treated groups. The secretion mechanisms of the treated parasites were impaired due to organic acids increased concentrations in the cysticerci. It is possible to conclude that the metabolic effect on alternative energetic pathways is slightly increased in the parasites treated with RCB20 than the ones treated with ABZSO.

The Omega Ring Imaging Cerenkov Detector readout system user's guide

International Nuclear Information System (INIS)

Hallewell, G.

1984-11-01

The manual describes the electronic readout system of the Ring Imaging Cerenkov Detector at the CERN Omega Spectrometer. The system is described in its configuration of September 1984 after the Rich readout system had been used in two Omega experiments. (U.K.)

Pulse radiolysis of 2-mercapto benzimidazole in aqueous solutions

Energy Technology Data Exchange (ETDEWEB)

Dey, G R; Naik, D B; Kishore, K; Moorthy, P N [Bhabha Atomic Research Centre, Bombay (India). Applied Chemistry Division

1994-12-31

The initial e{sub aq}{sup -}/H adducts of 2-mercapto benzimidazole(MBZ) ({lambda}{sub max} {approx} 370 nm) which are mild reductants react with parent compound to give an intermolecular 3-electron bonded species with {lambda}{sub max} at 590 nm. The rate constants for the reactions of MBZ with e{sub aq}{sup -} and OH radicals at pH 7 and with H-atoms at pH 2 were determined. OH radical reaction with MBZ gives an intramolecular 3-electron bonded species. (author). 2 refs., 2 figs., 1 tab.

Polymer/organosilica nanocomposites based on polyimide with benzimidazole linkages and reactive organoclay containing isoleucine amino acid: Synthesis, characterization and morphology properties

International Nuclear Information System (INIS)

Mallakpour, Shadpour; Dinari, Mohammad

2012-01-01

Highlights: ► A reactive organoclay was formed using L-isoleucine amino acid as a swelling agent. ► Polyimide was synthesized from benzimidazole diamine and pyromellitic dianhydride. ► Imide and benzimidazole groups assured the thermal stability of the nanocomposites. ► Nanocomposite films were prepared by an in situ polymerization reaction. ► The TEM micrographs of nanocomposites revealed well-exfoliated structures. -- Abstract: Polyimide–silica nanocomposites are attractive hybrid architectures that possess excellent mechanical, thermal and chemical properties. But, the dispersion of inorganic domains in the polymer matrix and the compatibility between the organic and inorganic phases are critical factors in these hybrid systems. In this investigation, a reactive organoclay was prepared via ion exchange reaction between protonated form of difunctional L-isoleucine amino acid as a swelling agent and Cloisite Na + montmorillonite. Amine functional groups of this swelling agent formed an ionic bond with the negatively charged silicates, whereas the remaining acid functional groups were available for further interaction with polymer chains. Then organo-soluble polyimide (PI) have been successfully synthesized from the reaction of 2-(3,5-diaminophenyl)-benzimidazole and pyromellitic dianhydride in N,N-dimethylacetamide. Finally, PI/organoclay nanocomposite films enclosing 1%, 3%, 5%, 7% and 10% of synthesized organoclay were successfully prepared by an in situ polymerization reaction through thermal imidization. The synthesized hybrid materials were subsequently characterized by Fourier transform infrared spectroscopy, X-ray diffraction, electron microscopy, and thermogravimetric analysis techniques. The PI/organoclay nanocomposite films have good optical transparencies and the mechanical properties were substantially improved by the incorporation of the reactive organoclay.

Synthesis, QSAR, and Molecular Dynamics Simulation of Amidino-substituted Benzimidazoles as Dipeptidyl Peptidase III Inhibitors.

Science.gov (United States)

Rastija, Vesna; Agić, Dejan; Tomiš, Sanja; Nikolič, Sonja; Hranjec, Marijana; Grace, Karminski-Zamola; Abramić, Marija

2015-01-01

A molecular modeling study is performed on series of benzimidazol-based inhibitors of human dipeptidyl peptidase III (DPP III). An eight novel compounds were synthesized in excellent yields using green chemistry approach. This study is aimed to elucidate the structural features of benzimidazole derivatives required for antagonism of human DPP III activity using Quantitative Structure-Activity Relationship (QSAR) analysis, and to understand the mechanism of one of the most potent inhibitor binding into the active site of this enzyme, by molecular dynamics (MD) simulations. The best model obtained includes S3K and RDF045m descriptors which have explained 89.4 % of inhibitory activity. Depicted moiety for strong inhibition activity matches to the structure of most potent compound. MD simulation has revealed importance of imidazolinyl and phenyl groups in the mechanism of binding into the active site of human DPP III.

Evaluation of the membrane permeability (PAMPA and skin) of benzimidazoles with potential cannabinoid activity and their relation with the Biopharmaceutics Classification System (BCS).

Science.gov (United States)

Alvarez-Figueroa, M Javiera; Pessoa-Mahana, C David; Palavecino-González, M Elisa; Mella-Raipán, Jaime; Espinosa-Bustos, Cristián; Lagos-Muñoz, Manuel E

2011-06-01

The permeability of five benzimidazole derivates with potential cannabinoid activity was determined in two models of membranes, parallel artificial membrane permeability assay (PAMPA) and skin, in order to study the relationship of the physicochemical properties of the molecules and characteristics of the membranes with the permeability defined by the Biopharmaceutics Classification System. It was established that the PAMPA intestinal absorption method is a good predictor for classifying these molecules as very permeable, independent of their thermodynamic solubility, if and only if these have a Log P(oct) value permeability is conditioned on the solubility of the molecule so that it can only serve as a model for classifying the permeability of molecules that possess high solubility (class I: high solubility, high permeability; class III: high solubility, low permeability).

Survey of Digital Feedback Systems in High Current Storage Rings

International Nuclear Information System (INIS)

Teytelman, Dmitry

2003-01-01

In the last decade demand for brightness in synchrotron light sources and luminosity in circular colliders led to construction of multiple high current storage rings. Many of these new machines require feedback systems to achieve design stored beam currents. In the same time frame the rapid advances in the technology of digital signal processing allowed the implementation of these complex feedback systems. In this paper I concentrate on three applications of feedback to storage rings: orbit control in light sources, coupled-bunch instability control, and low-level RF control. Each of these applications is challenging in areas of processing bandwidth, algorithm complexity, and control of time-varying beam and system dynamics. I will review existing implementations as well as comment on promising future directions

Pulsed rf systems for large storage rings

International Nuclear Information System (INIS)

Wilson, P.B.

1979-03-01

The possibility is considered that by using a pulsed rf system a substantial reduction can be made in the rf power requirement for the next generation of large storage rings. For a ring with a sufficiently large circumference, the time between bunch passages, T/sub b/, can exceed the cavity filling time, T/sub f/. As the ratio T/sub b//T/sub f/ increases, it is clear that at some point the average power requirement can be reduced by pulsing the rf to the cavities. In this mode of operation, the rf power is turned on a filling time or so before the arrival of a bunch and is switched off again at the time of bunch passage. There is no rf energy in the accelerating structure, and hence no power dissipation, for most of the period between bunches

Quantum-chemical insight into structure-reactivity relationship in 4,5,6,7-tetrahalogeno-1H-benzimidazoles: a combined X-ray, DSC, DFT/QTAIM, Hirshfeld surface-based, and molecular docking approach.

Science.gov (United States)

Latosińska, Jolanta Natalia; Latosińska, Magdalena; Maurin, Jan Krzysztof; Orzeszko, Andrzej; Kazimierczuk, Zygmunt

2014-03-20

The weak interaction patterns in 4,5,6,7-tetrahalogeno-1H-benzimidazoles, protein kinase CK2 inhibitors, in solid state are studied by the X-ray method and quantum chemistry calculations. The crystal structures of 4,5,6,7-tetrachloro- and 4,5,6,7-tetrabromo-1H-benzimidazole are determined by X-ray diffraction and refined to a final R-factor of 3.07 and 3.03%, respectively, at room temperature. The compound 4,5,6,7-tetrabromo-1H-benzimidazole, which crystallizes in the I41/a space group, is found to be isostructural with previously studied 4,5,6,7-tetraiodo-1H-benzimidazole in contrast to 4,5,6,7-tetrachloro-1H-benzimidazole, which crystallizes as triclinic P1̅ with 4 molecules in elementary unit. For 4,5,6,7-tetrachloro-1H-benzimidazole, differential scanning calorimetry (DSC) revealed a second order glassy phase transition at Tg = 95°/106° (heating/cooling), an indication of frozen disorder. The lack of 3D isostructurality found in all 4,5,6,7-tetrahalogeno-1H-benzimidazoles is elucidated on the basis of the intra- and intermolecular interactions (hydrogen bonding, van der Waals contacts, and C-H···π interactions). The topological Bader's Quantum Theory of Atoms in Molecules (QTAIM) and Spackman's Hirshfeld surface-based approaches reveal equilibration of electrostatic matching and dispersion van der Waals interactions between molecules consistent with the crystal site-symmetry. The weakening of van der Waals forces accompanied by increasing strength of the hydrogen bond (N-H···N) result in a decrease in the crystal site-symmetry and a change in molecular packing in the crystalline state. Crystal packing motifs were investigated with the aid of Hirshfeld surface fingerprint plots. The ordering 4,5,6,7-tetraiodo > 4,5,6,7-tetrabromo > 4,5,6,7-tetrachloro > 4,5,6,7-tetrafluoro reflects not only a decrease in crystal symmetry but also increase in chemical reactivity (electronic activation), which could explain some changes in biological activity of

Possibility of persistent voltage observation in a system of asymmetric superconducting rings

International Nuclear Information System (INIS)

Burlakov, A.A.; Gurtovoi, V.L.; Ilin, A.I.; Nikulov, A.V.; Tulin, V.A.

2012-01-01

The possibility of observing persistent voltage in superconducting rings of different arm widths is experimentally investigated. It was previously found that switching of the arms between superconducting and normal states by an AC current induces DC voltage oscillation in the magnetic field with a period corresponding to the flux quantum inside the ring. We used systems with a large number of asymmetric rings connected in series to investigate the possibility of observing this quantum phenomenon near the superconducting transition, where thermal fluctuations lead to switching of ring segments without an external influence and the persistent current is much smaller than in the superconducting state. -- Highlights: ► A possibility to observe the persistent voltage is investigated experimentally. ► The persistent voltage is a DC voltage observed at thermodynamic equilibrium. ► It oscillates in magnetic field like the persistent current in superconducting ring. ► The period of the oscillations corresponds to the flux quantum inside the ring. ► The quantum oscillations of the DC voltage were observed on asymmetric rings.

The structure and stability of orbits in Hoag-like ring systems

Science.gov (United States)

Bannikova, Elena Yu

2018-05-01

Ring galaxies are amazing objects exemplified by the famous case of Hoag's Object. Here the mass of the central galaxy may be comparable to the mass of the ring, making it a difficult case to model mechanically. In a previous paper, it was shown that the outer potential of a torus (ring) can be represented with good accuracy by the potential of a massive circle with the same mass. This approach allows us to simplify the problem of the particle motion in the gravitational field of a torus associated with a central mass by replacing the torus with a massive circle. In such a system, there is a circle of unstable equilibrium that we call `Lagrangian circle' (LC). Stable circular orbits exist only in some region limited by the last possible circular orbit related to the disappearance of the extrema of the effective potential. We call this orbit `the outermost stable circular orbit' (OSCO) by analogy with the innermost stable circular orbit (ISCO) in the relativistic case of a black hole. Under these conditions, there is a region between OSCO and LC where the circular motion is not possible due to the competition between the gravitational forces by the central mass and the ring. As a result, a gap in the matter distribution can form in Hoag-like system with massive rings.

Antibacterial activity of head-to-head bis-benzimidazoles.

Science.gov (United States)

Moreira, Joao B; Mann, John; Neidle, Stephen; McHugh, Timothy D; Taylor, Peter W

2013-10-01

Symmetric bis-benzimidazole (BBZ) conjugates were profiled for activity against a range of Gram-positive and Gram-negative bacteria. para-Substituted ethoxy, amino and methoxy derivatives displayed potent bacteriostatic activity against meticillin-resistant Staphylococcus aureus, vancomycin-resistant enterococci, streptococci and Listeria monocytogenes. Moderate to good activity was also found against mycobacteria; two compounds were strongly active against logarithmic phase and hypoxia-induced latent Mycobacterium tuberculosis. No compound displayed significant activity towards Gram-negative bacteria. Only high concentrations of antibacterial BBZs showed cytotoxic effects towards fibroblasts, and the most active compound was well tolerated by zebrafish embryos. Copyright © 2013 Elsevier B.V. and the International Society of Chemotherapy. All rights reserved.

Photometric and spectroscopic evidence for a dense ring system around Centaur Chariklo

Science.gov (United States)

Duffard, R.; Pinilla-Alonso, N.; Ortiz, J. L.; Alvarez-Candal, A.; Sicardy, B.; Santos-Sanz, P.; Morales, N.; Colazo, C.; Fernández-Valenzuela, E.; Braga-Ribas, F.

2014-08-01

Context. A stellar occultation observed on 3rd June 2013 revealed the presence of two dense and narrow rings separated by a small gap around the Centaur object (10 199) Chariklo. The composition of these rings is not known. We suspect that water ice is present in the rings, as is the case for Saturn and other rings around the giant planets. Aims: In this work, we aim to determine if the variability in the absolute magnitude of Chariklo and the temporal variation of the spectral ice feature, even when it disappeared in 2007, can be explained by an icy ring system whose aspect angle changes with time. Methods: We explained the variations on the absolute magnitude of Chariklo and its ring by modeling the light reflected by a system as the one described above. Using X-shooter at VLT, we obtained a new reflectance spectra. We compared this new set of data with the ones available in the literature. We showed how the water ice feature is visible in 2013 in accordance with the ring configuration, which had an opening angle of nearly 34° in 2013. Finally, we also used models of light scattering to fit the visible and near-infrared spectra that shows different characteristics to obtain information on the composition of Chariklo and its rings. Results: We showed that absolute photometry of Chariklo from the literature and new photometric data that we obtained in 2013 can be explained by a ring of particles whose opening angle changes as a function of time. We used the two possible pole solutions for the ring system and found that only one of them, α = 151.30 ± 0.5, δ = 41.48 ± 0.2° (λ = 137.9 ± 0.5, β = 27.7 ± 0.2°), provides the right variation of the aspect angle with time to explain the photometry, whereas the other possible pole solution fails to explain the photometry. From spectral modeling, we derived the composition of the Chariklo surface and that of the rings using the result on the pole solution. Chariklo surface is composed with about 60% of amorphous

Evaluating thermodynamic integration performance of the new amber molecular dynamics package and assess potential halogen bonds of enoyl-ACP reductase (FabI) benzimidazole inhibitors.

Science.gov (United States)

Su, Pin-Chih; Johnson, Michael E

2016-04-05

Thermodynamic integration (TI) can provide accurate binding free energy insights in a lead optimization program, but its high computational expense has limited its usage. In the effort of developing an efficient and accurate TI protocol for FabI inhibitors lead optimization program, we carefully compared TI with different Amber molecular dynamics (MD) engines (sander and pmemd), MD simulation lengths, the number of intermediate states and transformation steps, and the Lennard-Jones and Coulomb Softcore potentials parameters in the one-step TI, using eleven benzimidazole inhibitors in complex with Francisella tularensis enoyl acyl reductase (FtFabI). To our knowledge, this is the first study to extensively test the new AMBER MD engine, pmemd, on TI and compare the parameters of the Softcore potentials in the one-step TI in a protein-ligand binding system. The best performing model, the one-step pmemd TI, using 6 intermediate states and 1 ns MD simulations, provides better agreement with experimental results (RMSD = 0.52 kcal/mol) than the best performing implicit solvent method, QM/MM-GBSA from our previous study (RMSD = 3.00 kcal/mol), while maintaining similar efficiency. Briefly, we show the optimized TI protocol to be highly accurate and affordable for the FtFabI system. This approach can be implemented in a larger scale benzimidazole scaffold lead optimization against FtFabI. Lastly, the TI results here also provide structure-activity relationship insights, and suggest the parahalogen in benzimidazole compounds might form a weak halogen bond with FabI, which is a well-known halogen bond favoring enzyme. © 2015 Wiley Periodicals, Inc.

Differential sensing of fluoride and cyanide ions by using Dicyano substituted benzimidazole probe

Energy Technology Data Exchange (ETDEWEB)

Gupta, Akul Sen; Garg, Aparna; Paul, Kamaldeep; Luxami, Vijay, E-mail: vluxami@thapar.edu

2016-05-15

Excited State Intramolecular Proton Transfer based benzimidazole derivative having push–pull effect has been synthesized and investigated their photophysical behavior towards various anions. The probe 2 has been used for selective estimation of F{sup −} and CN{sup −} anions and signaled the binding event through formation of new absorption band at 465 nm. The probe 2 opens different emission channels at 425 nm in the presence of CN{sup −} ions and two new emission bands at 435 nm and 365 nm in case of F{sup −} ions. The probe 2 behaved as chemodosimeter for CN{sup −} ions which have been proved by {sup 1}H NMR and whereas fluoride caused hydrogen bonding interactions with probe 2 and restricted the ESIPT emission at 505 nm from OH to nitrogen of benzimidazole moiety to release its enol emission. The differential behavior of F{sup −} ions and CN{sup −} have been confirmed through DFT calculations. - Graphical abstract: The probe 2 binds chemodosimetrically with cyanide ions and act as chemosensor for fluoride ion.

Differential sensing of fluoride and cyanide ions by using Dicyano substituted benzimidazole probe

International Nuclear Information System (INIS)

Gupta, Akul Sen; Garg, Aparna; Paul, Kamaldeep; Luxami, Vijay

2016-01-01

Excited State Intramolecular Proton Transfer based benzimidazole derivative having push–pull effect has been synthesized and investigated their photophysical behavior towards various anions. The probe 2 has been used for selective estimation of F − and CN − anions and signaled the binding event through formation of new absorption band at 465 nm. The probe 2 opens different emission channels at 425 nm in the presence of CN − ions and two new emission bands at 435 nm and 365 nm in case of F − ions. The probe 2 behaved as chemodosimeter for CN − ions which have been proved by 1 H NMR and whereas fluoride caused hydrogen bonding interactions with probe 2 and restricted the ESIPT emission at 505 nm from OH to nitrogen of benzimidazole moiety to release its enol emission. The differential behavior of F − ions and CN − have been confirmed through DFT calculations. - Graphical abstract: The probe 2 binds chemodosimetrically with cyanide ions and act as chemosensor for fluoride ion.

The inflation of ion strength in the formation of co-ordination compounds in system of the Fe(III)-Fe(II)-benzimidazole-water in the 298 K

International Nuclear Information System (INIS)

Nazarova, Kh.D.; Rajabov, U.R.; Yusupov, Z.N.

2005-01-01

With the Method of Oxredmatrion with application of the Oxidation Function in the Temperature 298 K and ion strength 0.1; 0.25; 0.50 and 1.00 in the Water solution of Benzimidazole been obtained the Formation Constants of the Coordination and their dependence with ion strength

Potassium hydroxide/dimethyl sulfoxide promoted intramolecular cyclization for the synthesis of benzimidazol-2-ones.

Science.gov (United States)

Beyer, Astrid; Reucher, Christine M M; Bolm, Carsten

2011-06-03

A new protocol for intramolecular N-arylations of ureas to form benzimidazol-2-ones has been developed. The cyclization reaction occurs in the presence of KOH and DMSO at close to ambient temperature. Under these conditions the yields are high and a wide range of functional groups are tolerated.

Characterizing exo-ring systems around fast-rotating stars using the Rossiter-McLaughlin effect

Science.gov (United States)

de Mooij, Ernst J. W.; Watson, Christopher A.; Kenworthy, Matthew A.

2017-12-01

Planetary rings produce a distinct shape distortion in transit light curves. However, to accurately model such light curves the observations need to cover the entire transit, especially ingress and egress, as well as an out-of-transit baseline. Such observations can be challenging for long period planets, where the transits may last for over a day. Planetary rings will also impact the shape of absorption lines in the stellar spectrum, as the planet and rings cover different parts of the rotating star (the Rossiter-McLaughlin effect). These line-profile distortions depend on the size, structure, opacity, obliquity and sky-projected angle of the ring system. For slow-rotating stars, this mainly impacts the amplitude of the induced velocity shift; however, for fast-rotating stars the large velocity gradient across the star allows the line distortion to be resolved, enabling direct determination of the ring parameters. We demonstrate that by modelling these distortions we can recover ring system parameters (sky-projected angle, obliquity and size) using only a small part of the transit. Substructure in the rings, e.g. gaps, can be recovered if the width of the features (δW) relative to the size of the star is similar to the intrinsic velocity resolution (set by the width of the local stellar profile, γ) relative to the stellar rotation velocity (v sini, i.e. δW/R* ≳ vsini/γ). This opens up a new way to study the ring systems around planets with long orbital periods, where observations of the full transit, covering the ingress and egress, are not always feasible.

Design considerations for a feedback system to control self-bunching in ion-storage rings

International Nuclear Information System (INIS)

Ziemann, V.

2001-02-01

We discuss the feasibility of a feedback system to cure self-bunching of the electron-cooled coasting ion-beam in CELSIUS. Such a system may also aid stable operation of accumulator rings for future spallation neutron sources or heavy ion rings used for inertial fusion energy production

Novel product ions of 2-aminoanilide and benzimidazole Ag(I) complexes using electrospray ionization with multi-stage tandem mass spectrometry.

Science.gov (United States)

Johnson, Byron S; Burinsky, David J; Burova, Svetlana A; Davis, Roman; Fitzgerald, Russ N; Matsuoka, Richard T

2012-05-15

The 2-aminoaniline scaffold is of significant value to the pharmaceutical industry and is embedded in a number of pharmacophores including 2-aminoanilides and benzimidazoles. A novel application of coordination ion spray mass spectrometry (CIS-MS) for interrogating the silver ion (Ag(+)) complexes of a homologous series of these compounds using multi-stage tandem mass spectrometry is described. Unlike the ubiquitous alkali metal ion complexes, Ag(+) complexes of 2-aminoanilides and benzimidazoles were found to yield [M - H](+) ions in significant abundance via gas-phase elimination of the metal hydride (AgH) resulting in unique product ion cascades. Sample introduction was by liquid chromatography with mass spectrometry analysis performed on a hybrid linear ion trap/orbitrap instrument capable of high-resolution measurements. Rigorous structural characterization by multi-stage tandem mass spectrometry using [M +  H](+), [M - H](-) and [M - H](+) precursor ions derived from ESI and CIS experiments was performed for the homologous series of 2-aminoanilide and benzimidazole compounds. A full tabular comparison of structural information resulting from these product ion cascades was produced. Multi-stage tandem mass spectrometry of [M - H](+) ions resulting from Ag(+) complexes of 2-aminoanilides and benzimidazoles in CIS-MS experiments produced unique product ion cascades that exhibited complementary structural information to that obtained from tandem mass spectrometry of [M  +  H](+) and [M - H](-) ions by electrospray ionization (ESI). These observations may be broadly applicable to other compounds that are observed to form Ag(+) complexes and eliminate AgH. Copyright © 2012 John Wiley & Sons, Ltd.

Development of novel (1-H benzimidazole bearing pyrimidine-trione based MAO-A inhibitors: Synthesis, docking studies and antidepressant activity

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Bijo Mathew

2016-09-01

Full Text Available The synthesis of some novel (1-H benzimidazole bearing pyrimidine-trione based MAO-A inhibitors were achieved by the reaction between 2E-1-(1H-benzimidazol-2-yl-3-phenylprop-2-en-1-ones(4a–f and barbituric acid in the presence of a catalytic amount of acetic acid medium. All the final structures were assigned on the basis of IR, 1HNMR and mass spectra analyses. All the synthesized derivatives showed good antidepressant activity when compared to the standard clomipiramine at a dose level of 20 mg/kg. The compound (5d 5-{(2E-1-(1H-benzimidazol-2-yl-3-[4-(dimethylaminophenyl] prop-2-en-1-ylidene} pyrimidine-2, 4, 6(1H,3H,5H-trione significantly reduced the duration of immobility times at 50 mg/kg−1 dose level when compared to the standard drug. Molecular docking studies revealed the need for an extra hydrophobic interaction in the titled scaffold for acquiring the promising experimental values. It has been concluded that the computational values obtained after the docking calculation are in good agreement with the experimental values.

Investigation into organic boron compounds complexing. 25. Triaryl borane complexes with benzimidazole

Energy Technology Data Exchange (ETDEWEB)

Belonovich, M I; Lapkin, I I; Morozova, T L; Okatysheva, L Yu; Rybakova, M N; Yuzhakova, G A [Permskij Gosudarstvennyj Univ. (USSR)

1984-02-01

Coordination of organic boron compounds with heterocyclic ligands is studied. Substances containing one molecule of ligand per one molecule of triarylborane are extracted when mixing ether solution of triarylborane and alcohol solution of benzimidazole. Based on IR spectra it is stated that coordination with boron is realized at the expense of pyridine nitrogen atom of imidazole cycle. Dipole momenta are determined for synthesized complexes using Debye method.

Cellular distribution, purification and electrophoretic properties of malate dehydrogenase in Trichuris ovis and inhibition by benzimidazoles and pyrimidine derivatives.

Science.gov (United States)

Sanchez-Moreno, M; Ortega, J E; Valero, A

1989-12-01

High levels of malate dehydrogenase were found in Trichuris ovis. Two molecular forms of the enzyme, of different cellular location and electrophoretic pattern, were isolated and purified. The activity of soluble malate dehydrogenase was greater than that of mitochondrial malate dehydrogenase. Both forms also displayed different electrophoretic profiles in comparison with purified extracts from goat (Capra hircus) liver. Substrate concentration directly affected enzyme activity. Host and parasite malate dehydrogenase activity were both inhibited by a series of benzimidazoles and pyrimidine-derived compounds, some of which markedly reduced parasite enzyme activity, but not host enzyme activity. Percentage inhibition by some pyrimidine derivatives was greater than that produced by benzimidazoles.

Synthesis and properties of poly(aryl sulfone benzimidazole) and its copolymers for high temperature membrane electrolytes for fuel cells

DEFF Research Database (Denmark)

Yang, Jingshuai; Li, Qingfeng; Cleemann, Lars Nilausen

2012-01-01

Poly(aryl sulfone benzimidazole) (SO2PBI) and its copolymers with poly[2,2′-p-(phenylene)-5,5′-bibenzimidazole] (pPBI), termed as Co-SO2PBI, were synthesized with varied feeding ratios of 4,4′-sulfonyldibenzoic acid (SDBA) to terephthalic acid (TPA). Incorporation of the stiff para-phenylene and ......Poly(aryl sulfone benzimidazole) (SO2PBI) and its copolymers with poly[2,2′-p-(phenylene)-5,5′-bibenzimidazole] (pPBI), termed as Co-SO2PBI, were synthesized with varied feeding ratios of 4,4′-sulfonyldibenzoic acid (SDBA) to terephthalic acid (TPA). Incorporation of the stiff para...

Relationship of Resistance to Benzimidazole Fungicides with Mutation of β-Tubulin Gene in Venturia nashicola

Directory of Open Access Journals (Sweden)

Yeonsoo Kwak

2017-06-01

Full Text Available Pear scab caused by Venturia nashicola has been reported as an important disease of pear resulting in lowering the quality of pear fruits. In this study, it was conducted to investigate the relationship between resistance of V. nashicola and mutation of β-tubulin gene and the fungicide resistance in field isolate group in benzimidazole fungicides. Responce of V. nashicola to carbendazim could be classified into 3 groups as sensitive that does not grow at all on PDA amended with 0.16 μg/ml of carbendazim, low resistance that could not grow in 4.0 μg/ml medium, and high resistance that can grow even at 100 μg/ml. Thirty isolates of V. nashicola collected from 3 regions as Wonju, Naju, and Okcheon were highly resistant to carbendazim. Analysis of the nucleotide sequence of β-tubulin gene of V. nashicola showed that there was no difference in the nucleotide sequence between the sensitive and the low-resistant isolate, but GAG at codon 198 (glutamic acid was replaced with GCG (alanine in the high-resistant isolate. Among 10 isolates obtained from the Okcheon, 5 isolates showed the substitution of glycine for glutamic acid, which were resistant to carbendazim, but more sensitive to the mixture of carbendazim and diethofencarb than others. Through these results, all isolates of V. nashicola isolated in pear orchard were found to be resistant to benzimidazoles. Also, mutants E198A and E198G at β-tubulin were found to be important mechanisms of V. nashicola resistance against benzimidazole fungicides.

On the Aharonov-Casher system and the Landau-Aharonov-Casher system confined to a two-dimensional quantum ring

International Nuclear Information System (INIS)

Bakke, K.; Furtado, C.

2012-01-01

We study the quantum dynamics of a neutral particle in the Aharonov-Casher system and in the Landau-Aharonov-Casher system confined to a two-dimensional quantum ring, a quantum dot, and a quantum anti-dot potentials described by the Tan-Inkson model [W.-C. Tan and J. C. Inkson, Semicond. Sci. Technol. 11, 1635 (1996)]. We show, in the Aharonov-Casher system, that bound states can be achieved when the neutral particle is confined to the two-dimensional quantum ring and the quantum dot and discuss the appearance of persistent currents. In the Landau-Aharonov-Casher system, we show that bound states can be achieved when the neutral particle is confined to the quantum anti-dot, quantum dot, and the two-dimensional quantum ring, but there are no persistent currents.

Silica Sulfuric Acid: An Eco-Friendly and Reusable Catalyst for Synthesis of Benzimidazole Derivatives

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Bahareh Sadeghi

2013-01-01

Full Text Available Silica sulfuric acid (SiO2-OSO3H as an eco-friendly, readily available, and reusable catalyst is applied to benzimidazole derivatives synthesis under reflux in ethanol. The procedure is very simple and the products are isolated with an easy workup in good-to-excellent yields.

Numerical study on the lubrication performance of compression ring-cylinder liner system with spherical dimples.

Directory of Open Access Journals (Sweden)

Cheng Liu

Full Text Available The effects of surface texture on the lubrication performance of a compression ring-cylinder liner system are studied in this paper. By considering the surface roughness of the compression ring and cylinder liner, a mixed lubrication model is presented to investigate the tribological behaviors of a barrel-shaped compression ring-cylinder liner system with spherical dimples on the liner. In order to determine the rupture and reformulation positions of fluid film accurately, the Jacoboson-Floberg-Olsson (JFO cavitation boundary condition is applied to the mixed lubrication model for ensuring the mass-conservative law. On this basis, the minimum oil film thickness and average friction forces in the compression ring-cylinder liner system are investigated under the engine-like conditions by changing the dimple area density, radius, and depth. The wear load, average friction forces, and power loss of the compression ring-cylinder liner system with and without dimples are also compared for different compression ring face profiles. The results show that the spherical dimples can produce a larger reduction of friction in mixed lubrication region, and reduce power loss significantly in the middle of the strokes. In addition, higher reduction percentages of average friction forces and wear are obtained for smaller crown height or larger axial width.

Phosphorylated benzimedazoles. 8. Synthesis of phosphorylated with /sup 32/P benzimidazoles

Energy Technology Data Exchange (ETDEWEB)

Makarov, A M; Matevosyan, G L; Zavlin, P M [Leningradskij Sel' skokhozyajstvennyj Inst. (USSR)

1983-03-01

Accessible methods of synthesis and identification of phosphorylated benzimidazoles with specific activity close to the maximum permissible with labelled /sup 32/P are developed. These methods permit to determine the permissible residual amounts of the above preparations in nutrition products and the maximum permissible amounts of growth regulators in different objects of the environment, because it is impossible to detect, for example, tri(1-benzimidazolido)phosphate with other physico-chemical methods with the existing concentration of 10/sup -9/%.

Real-time track-less Cherenkov ring fitting trigger system based on Graphics Processing Units

Science.gov (United States)

Ammendola, R.; Biagioni, A.; Chiozzi, S.; Cretaro, P.; Cotta Ramusino, A.; Di Lorenzo, S.; Fantechi, R.; Fiorini, M.; Frezza, O.; Gianoli, A.; Lamanna, G.; Lo Cicero, F.; Lonardo, A.; Martinelli, M.; Neri, I.; Paolucci, P. S.; Pastorelli, E.; Piandani, R.; Piccini, M.; Pontisso, L.; Rossetti, D.; Simula, F.; Sozzi, M.; Vicini, P.

2017-12-01

The parallel computing power of commercial Graphics Processing Units (GPUs) is exploited to perform real-time ring fitting at the lowest trigger level using information coming from the Ring Imaging Cherenkov (RICH) detector of the NA62 experiment at CERN. To this purpose, direct GPU communication with a custom FPGA-based board has been used to reduce the data transmission latency. The GPU-based trigger system is currently integrated in the experimental setup of the RICH detector of the NA62 experiment, in order to reconstruct ring-shaped hit patterns. The ring-fitting algorithm running on GPU is fed with raw RICH data only, with no information coming from other detectors, and is able to provide more complex trigger primitives with respect to the simple photodetector hit multiplicity, resulting in a higher selection efficiency. The performance of the system for multi-ring Cherenkov online reconstruction obtained during the NA62 physics run is presented.

Resistance to benzimidazoles and levamisole in nematode parasites of sheep in Nyandarua district of Kenya

DEFF Research Database (Denmark)

Maingi, N.; Bjørn, H.; Gichohi, V.M.

1998-01-01

The occurrence of anthelmintic resistance on 25 sheep farms in the Nyandarua District of Kenya was investigated, using the faecal egg count reduction test (FECRT), the egg hatch assay (EHA) and a larval development assay (LDA). In the FECRT, resistance to both benzimidazoles (BZs) and levamisole...

Nanostructured poly(benzimidazole membranes by N-alkylation

Directory of Open Access Journals (Sweden)

J. Weber

2014-01-01

Full Text Available Modification of poly(benzimidazole (PBI by N-alkylation leads to polymers capable of undergoing microphase separation. Polymers with different amounts of C18 alkyl chains have been prepared. The polymers were analyzed by spectroscopy, thermal analysis, electron microscopy and X-ray scattering. The impact of the amount of alkyl chains on the observed microphase separation was analyzed. Membranes prepared from the polymers do show microphase separation, as evidenced by scattering experiments. While no clear morphology could be derived for the domains in the native state, evidence for the formation of lamellar morphologies upon doping with phosphoric acid is provided. Finally, the proton conductivity of alkyl-modified PBI is compared with that of pure PBI, showing that the introduction of alkyl side chains does not result in significant conductivity changes.

A Study of Storage Ring Requirements for an Explosive Detection System Using NRA Method.

Energy Technology Data Exchange (ETDEWEB)

Wang, T. F. (Tai-Sen F.); Kwan, T. J. T. (Thomas J. T.)

2005-01-01

The technical feasibility of an explosives detection system based on the nuclear resonance absorption (NRA) of gamma rays in nitrogen-rich materials was demonstrated at Los Alamos National Laboratory (LANL) in 1993 by using an RFQ proton accelerator and a tomographic imaging prototype. The study is being continued recently to examine deployment of such an active interrogation system in realistic scenarios. The approach is to use an accelerator and electron-cooling-equipped storage rings(s) to provide the high quality and high current proton beam needed in a practical application. In this work, we investigate the requirements on the storage ring(s) with external gamma-ray-production target for a variant of the airport luggage inspection system considered in the earlier LANL experiments. Estimations are carried out based on the required inspection throughput, the gamma ray yield, the proton beam emittance growth due to scatters with the photon-production target, beam current limit in the storage ring, and the electron-cooling rate. Studies using scaling and reasonable parameter values indicate that it is possible to use no more than a few storage rings per inspection station in a practical NRA luggage inspection complex having more than ten inspection stations.

Study of RF system of Hefei storage ring under injection

International Nuclear Information System (INIS)

Xu Hongliang; Wang Lin; Li Yongjun; Huang Guirong; Zhang Pengfei; Li Weimin; Liu Zuping; He Duohui

2004-01-01

In this paper, the beam loading effect of RF system and the conditions of Robinson instability are analyzed in detail. By the study of the injection beam intensity limit dependent on detune angle and visible detune angle, it is found that the storage ring can be injected to more than 300 mA current intensity to attain the design target of phase II project in the lower energy injection situation of Hefei Storage Ring if a certain power is feed in the RF cavity and a certain tuning angle of the RF cavity is set

Proton-conducting membranes based on benzimidazole-containing sulfonated poly(ether ether ketone) compared with their carboxyl acid form

Energy Technology Data Exchange (ETDEWEB)

Li, Hongtao; Wu, Jing; Zhao, Chengji; Zhang, Gang; Zhang, Yang; Shao, Ke; Xu, Dan; Lin, Haidan; Han, Miaomiao; Na, Hui [Alan G MacDiarmid Institute, College of Chemistry, Jilin University, Changchun 130012 (China)

2009-10-15

A series of sulfonated poly(ether ether ketone) containing pendant carboxyl (C-SPEEKs) have been synthesized using a nucleophilic polycondesation reaction. A condensation reaction between 1,2-diaminobenzene and carboxyl resulted in a new series of copolymers containing benzimidazole groups (SPEEK-BIms). The expected structures of the sulfonated copolymers are confirmed by {sup 1}H NMR. The dependence of ion exchange capacity, water uptake, proton conductivity and methanol diffusion coefficient of SPEEK-BIm membranes has been studied and compared with their carboxyl acid form. The results suggest that the introduction of benzimidazole groups may be responsible for many excellent properties of the membranes for fuel cell. It is noticeable that the markedly improved oxidative stability is benefit for the application of membrane. (author)

Structure and dynamics of ringed galaxies

International Nuclear Information System (INIS)

Buta, R.J.

1984-01-01

In many spiral and SO galaxies, single or multiple ring structures are visible in the disk. These inner rings (r), outer rings (R), and nuclear rings (nr) were investigated by means of morphology, photometry, and spectroscopy in order to provide basic data on a long neglected phenomenon. The metric properties of each ring are investigated and found to correlate with the structure of the parent galaxy. When properly calibrated, inner rings in barred (SB) systems can be used as geometric extragalactic distance indicators to distances in excess of 100 Mpc. Other statistics are presented that confirm previous indications that the rings have preferred shapes, relative sizes, and orientations with respect to bars. A survey is made of the less homogeneous non-barred (SA) ringed systems, and the causes of the inhomogeneity are isolated. It is shown that rings can be identified in multiple-ring SA systems that are exactly analogous to those in barred spirals

Highly efficient water-mediated approach to access benzazoles: metal catalyst and base-free synthesis of 2-substituted benzimidazoles, benzoxazoles, and benzothiazoles.

Science.gov (United States)

Bala, Manju; Verma, Praveen Kumar; Sharma, Deepika; Kumar, Neeraj; Singh, Bikram

2015-05-01

An efficient water-catalyzed method has been developed for the synthesis of 2-substituted benzimidazoles, benzoxazoles, and benzothiazoles in one step. The present method excludes the usage of toxic metal catalysts and bases to produce benzazoles in good to excellent yields. An efficient and versatile water-mediated method has been established for the synthesis of various 2-arylbenzazoles. The present protocol excludes the usage of any catalyst and additive provided excellent selectivities and yields with high functional group tolerance for the synthesis of 2-arylated benzimidazoles, benzoxazoles, and benzothiazoles. Benzazolones were also synthesized using similar reaction protocol.

QSAR Analysis of 2-Amino or 2-Methyl-1-Substituted Benzimidazoles Against Pseudomonas aeruginosa

Science.gov (United States)

Podunavac-Kuzmanović, Sanja O.; Cvetković, Dragoljub D.; Barna, Dijana J.

2009-01-01

A set of benzimidazole derivatives were tested for their inhibitory activities against the Gram-negative bacterium Pseudomonas aeruginosa and minimum inhibitory concentrations were determined for all the compounds. Quantitative structure activity relationship (QSAR) analysis was applied to fourteen of the abovementioned derivatives using a combination of various physicochemical, steric, electronic, and structural molecular descriptors. A multiple linear regression (MLR) procedure was used to model the relationships between molecular descriptors and the antibacterial activity of the benzimidazole derivatives. The stepwise regression method was used to derive the most significant models as a calibration model for predicting the inhibitory activity of this class of molecules. The best QSAR models were further validated by a leave one out technique as well as by the calculation of statistical parameters for the established theoretical models. To confirm the predictive power of the models, an external set of molecules was used. High agreement between experimental and predicted inhibitory values, obtained in the validation procedure, indicated the good quality of the derived QSAR models. PMID:19468332

Adsorption and desorption characteristic of benzimidazole based fungicide carbendazim in pakistani soils

International Nuclear Information System (INIS)

Ahmad, K.S.; Rashid, N.; Tazaiyen, S.; Nazar, M.F.

2013-01-01

A versatile cost-effective Benzimidazole based fungicide, Carbendazim (methyl 1H-benzimidazole-2 carboxylate ) has been utilized to investigate its sorption-desorption behaviour on physicochemical properties of geographical soils, ranging from hilly to desert areas of Pakistan, via batch equilibrium method. The data obtained in all tests showed that adsorption co-efficient isotherm for Carbendazim in four tested soil were well fitted the freundlich equation. Distribution co-efficient (K d ) parameters are low (3.59 to 11.60 ml micro g/sup -1/) indicating low adsorption. It was observed that Carbendazim showed a relatively greater degree of adsorption on soil samples (Soil 4) that were collected from northern hilly areas Ayubia, Khyber Pakhton khaw (KPK) (Silt loam) i.e.11.60 ml mu g/sup -1/ and least adsorption on sandy Soil of Multan Punjab(Soil 2). While other two soils 1 were collected from Murree region, a boarder of Punjab and KPK mountain area and Soil 3 from Tarnol, Islamabad. Desorption studies reveal that the adsorbed fungicide is firmly retained by soil particles and their adsorption are almost irreversible. The results indicate that soil organic matter (SOM) and appropriate pH also play key role in sorption capacity. (author)

Design and Synthesis of Benzimidazoles As Novel Corticotropin-Releasing Factor 1 Receptor Antagonists.

Science.gov (United States)

Mochizuki, Michiyo; Kori, Masakuni; Kobayashi, Katsumi; Yano, Takahiko; Sako, Yuu; Tanaka, Maiko; Kanzaki, Naoyuki; Gyorkos, Albert C; Corrette, Christopher P; Cho, Suk Young; Pratt, Scott A; Aso, Kazuyoshi

2016-03-24

Benzazole derivatives with a flexible aryl group bonded through a one-atom linker as a new scaffold for a corticotropin-releasing factor 1 (CRF1) receptor antagonist were designed, synthesized, and evaluated. We expected that structural diversity could be expanded beyond that of reported CRF1 receptor antagonists. In a structure-activity relationship study, 4-chloro-N(2)-(4-chloro-2-methoxy-6-methylphenyl)-1-methyl-N(7),N(7)-dipropyl-1H-benzimidazole-2,7-diamine 29g had the most potent binding activity against a human CRF1 receptor and the antagonistic activity (IC50 = 9.5 and 88 nM, respectively) without concerns regarding cytotoxicity at 30 μM. Potent CRF1 receptor-binding activity in brain in an ex vivo test and suppression of stress-induced activation of the hypothalamus-pituitary-adrenocortical (HPA) axis were also observed at 138 μmol/kg of compound 29g after oral administration in mice. Thus, the newly designed benzimidazole 29g showed in vivo CRF1 receptor antagonistic activity and good brain penetration, indicating that it is a promising lead for CRF1 receptor antagonist drug discovery research.

An innovative seismic bracing system based on a superelastic shape memory alloy ring

International Nuclear Information System (INIS)

Gao, Nan; Jeon, Jong-Su; DesRoches, Reginald; Hodgson, Darel E

2016-01-01

Shape memory alloys (SMAs) have great potential in seismic applications because of their remarkable superelasticity. Seismic bracing systems based on SMAs can mitigate the damage caused by earthquakes. The current study investigates a bracing system based on an SMA ring which is capable of both re-centering and energy dissipation. This lateral force resisting system is a cross-braced system consisting of an SMA ring and four tension-only cable assemblies, which can be applied to both new construction and seismic retrofit. The performance of this bracing system is examined through a quasi-static cyclic loading test and finite element (FE) analysis. This paper describes the experimental design in detail, discusses the experimental results, compares the performance with other bracing systems based on SMAs, and presents an Abaqus FE model calibrated on the basis of experimental results to simulate the superelastic behavior of the SMA ring. The experimental results indicate that the seismic performance of this system is promising in terms of damping and re-centering. The FE model can be used in the simulation of building structures using the proposed bracing system. (paper)

Development of a circular shape Si-PM-based detector ring for breast-dedicated PET system

Science.gov (United States)

Nakanishi, Kouhei; Yamamoto, Seiichi; Watabe, Hiroshi; Abe, Shinji; Fujita, Naotoshi; Kato, Katsuhiko

2018-02-01

In clinical situations, various breast-dedicated positron emission tomography (PET) systems have been used. However, clinical breast-dedicated PET systems have polygonal detector ring. Polygonal detector ring sometimes causes image artifact, so complicated reconstruction algorithm is needed to reduce artifact. Consequently, we developed a circular detector ring for breast-dedicated PET to obtain images without artifact using a simple reconstruction algorithm. We used Lu1.9Gd0.1SiO5 (LGSO) scintillator block which was made of 1.5 x 1.9 x 15 mm pixels that were arranged in an 8 x 24 matrix. As photodetectors, we used silicon photomultiplier (Si-PM) arrays whose channel size was 3 x 3 mm. A detector unit was composed of four scintillator blocks, 16 Si-PM arrays and a light guide. The developed detector unit had angled configuration since the light guide was bending. A detector unit had three gaps with an angle of 5.625° between scintillator blocks. With these configurations, we could arrange 64 scintillator blocks in nearly circular shape (regular 64-sided polygon) using 16 detector units. The use of the smaller number of detector units could reduce the size of the front-end electronics circuits. The inner diameter of the developed detector ring was 260 mm. This size was similar to those of brain PET systems, so our breast-dedicated PET detector ring can measure not only breast but also brain. Measured radial, tangential and axial spatial resolution of the detector ring reconstructed by the filtered back-projection (FBP) algorithm were 2.1 mm FWHM, 2.0 mm FWHM and 1.7 mm FWHM at center of field of view (FOV), respectively. The sensitivity was 2.0% at center of the axial FOV. With the developed detector ring, we could obtain high resolution image of the breast phantom and the brain phantom. We conclude that our developed Si-PM-based detector ring is promising for a high resolution breast-dedicated PET system that can also be used for brain PET system.

Facile and Selective Synthesis of 2-Substituted Benzimidazoles Catalyzed by FeCl3/ Al2O3

Directory of Open Access Journals (Sweden)

Guo-Feng Chen

2012-01-01

Full Text Available 2-Substituted benzimidazoles were synthesized in a single pot from aromatic aldehydes and o-phenylenediamine catalyzed by FeCl3/ Al2O3 in DMF at ambient temperature attained good yields and high selectivity.

Planetary Rings

Science.gov (United States)

Nicholson, P. D.

2001-11-01

A revolution in the studies in planetary rings studies occurred in the period 1977--1981, with the serendipitous discovery of the narrow, dark rings of Uranus, the first Voyager images of the tenuous jovian ring system, and the many spectacular images returned during the twin Voyager flybys of Saturn. In subsequent years, ground-based stellar occultations, HST observations, and the Voyager flybys of Uranus (1986) and Neptune (1989), as well as a handful of Galileo images, provided much additional information. Along with the completely unsuspected wealth of detail these observations revealed came an unwelcome problem: are the rings ancient or are we privileged to live at a special time in history? The answer to this still-vexing question may lie in the complex gravitational interactions recent studies have revealed between the rings and their retinues of attendant satellites. Among the four known ring systems, we see elegant examples of Lindblad and corotation resonances (first invoked in the context of galactic disks), electromagnetic resonances, spiral density waves and bending waves, narrow ringlets which exhibit internal modes due to collective instabilities, sharp-edged gaps maintained via tidal torques from embedded moonlets, and tenuous dust belts created by meteoroid impact onto parent bodies. Perhaps most puzzling is Saturn's multi-stranded, clumpy F ring, which continues to defy a simple explanation 20 years after it was first glimpsed in grainy images taken by Pioneer 11. Voyager and HST images reveal a complex, probably chaotic, dynamical interaction between unseen parent bodies within this ring and its two shepherd satellites, Pandora and Prometheus. The work described here reflects contributions by Joe Burns, Jeff Cuzzi, Luke Dones, Dick French, Peter Goldreich, Colleen McGhee, Carolyn Porco, Mark Showalter, and Bruno Sicardy, as well as those of the author. This research has been supported by NASA's Planetary Geology and Geophysics program and the

Pharmacological evaluation of halogenated and non-halogenated arylpiperazin-1-yl-ethyl-benzimidazoles as D(2) and 5-HT(2A) receptor ligands.

Science.gov (United States)

Tomić, Mirko; Vasković, Djurdjica; Tovilović, Gordana; Andrić, Deana; Penjišević, Jelena; Kostić-Rajačić, Sladjana

2011-05-01

Five groups of previously synthesized and initially screened non-substituted and 4-halogenated arylpiperazin-1-yl-ethyl-benzimidazoles were estimated for their in-vitro binding affinities at the rat D(2) , 5-HT(2A) , and α(1) -adrenergic receptors. Among all these compounds, 2-methoxyphenyl and 2-chlorophenyl piperazines demonstrate the highest affinities for the tested receptors. The effects of 4-halogenation of benzimidazoles reveal that substitution with bromine may greatly increase the affinity of the compounds for the studied receptors, while the effect of substitution with chlorine is less remarkable. Most of the tested components show 5-HT(2A)/D(2) pK(i) binding ratios slightly above or less than 1, while only 4-chloro-6-(2-{4-[3-(trifluoromethyl)phenyl]piperazin-1-yl}ethyl)-1H-benzimidazole expresses an appropriate higher binding ratio (1.14), which was indicated for atypical neuroleptics. This compound exhibits a non-cataleptic action in rats and prevents d-amphetamine-induced hyperlocomotion in mice, which suggest its atypical antipsychotic potency. Copyright © 2011 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

Polyethylene glycol (PEG-400: An efficient medium for the synthesis of 1,2-disubstituted benzimidazoles

Directory of Open Access Journals (Sweden)

Raja Sekhar Mekala

2015-12-01

Full Text Available Polyethylene glycol (PEG-400 was found to be an inexpensive, non-toxic, and effective medium for the one-pot synthesis of 1,2-disubstituted benzimidazoles in excellent yields. Eco-friendliness, low cost, high yields, and recyclability of the PEG-400 are the important features of this protocol.

The beam loss monitoring system for HLS storage ring

CERN Document Server

Li Yu Xiong; Li Wei; Li Jue Xin; Liu Zu Ping; Shao Bei Bei

2001-01-01

A beam loss monitoring system has been established at HLS. This paper gives its principle and scientific grounds. Study on the ring's TBA structure and utilization of Monte-Carlo calculation to the shower electrons is important in its design. The system composition and performance are also introduced. The detector BLMs, data acquisition devices and host PC are linked via CAN bus. This system is helpful to analyze beam loss distribution and regulate the machine operation parameters.

Auto-production of biosurfactants reverses the coffee ring effect in a bacterial system

Science.gov (United States)

Sempels, Wouter; de Dier, Raf; Mizuno, Hideaki; Hofkens, Johan; Vermant, Jan

2013-04-01

The deposition of material at the edge of evaporating droplets, known as the ‘coffee ring effect’, is caused by a radially outward capillary flow. This phenomenon is common to a wide array of systems including colloidal and bacterial systems. The role of surfactants in counteracting these coffee ring depositions is related to the occurrence of local vortices known as Marangoni eddies. Here we show that these swirling flows are universal, and not only lead to a uniform deposition of colloids but also occur in living bacterial systems. Experiments on Pseudomonas aeruginosa suggest that the auto-production of biosurfactants has an essential role in creating a homogeneous deposition of the bacteria upon drying. Moreover, at biologically relevant conditions, intricate time-dependent flows are observed in addition to the vortex regime, which are also effective in reversing the coffee ring effect at even lower surfactant concentrations.

DNA-Compatible Nitro Reduction and Synthesis of Benzimidazoles.

Science.gov (United States)

Du, Huang-Chi; Huang, Hongbing

2017-10-18

DNA-encoded chemical libraries have emerged as a cost-effective alternative to high-throughput screening (HTS) for hit identification in drug discovery. A key factor for productive DNA-encoded libraries is the chemical diversity of the small molecule moiety attached to an encoding DNA oligomer. The library structure diversity is often limited to DNA-compatible chemical reactions in aqueous media. Herein, we describe a facile process for reducing aryl nitro groups to aryl amines. The new protocol offers simple operation and circumvents the pyrophoric potential of the conventional method (Raney nickel). The reaction is performed in aqueous solution and does not compromise DNA structural integrity. The utility of this method is demonstrated by the versatile synthesis of benzimidazoles on DNA.

Impact of zeolite-Y framework on the geometry and reactivity of Ru (III) benzimidazole complexes - A DFT study

Science.gov (United States)

Selvaraj, Tamilmani; Rajalingam, Renganathan; Balasubramanian, Viswanathan

2018-03-01

A detailed comparative Density Functional Theory (DFT) study is made to understand the structural changes of the guest complex due to steric and electronic interactions with the host framework. In this study, Ru(III) benzimidazole and 2- ethyl Ru(III) benzimidazole complexes encapsulated in a supercage of zeolite Y. The zeolitic framework integrity is not disturbed by the intrusion of the large guest complex. A blue shift in the d-d transition observed in the UV-Visible spectroscopic studies of the zeolite encapsulated complexes and they shows a higher catalytic efficiency. Encapsulation of zeolite matrix makes the metal center more viable to nucleophilic attack and favors the phenol oxidation reaction. Based on the theoretical calculations, transition states and structures of reaction intermediates involved in the catalytic cycles are derived.

Synthesis and PASS-assisted in silico approach of some novel 2-substituted benzimidazole bearing a pyrimidine-2, 4, 6(trione system as mucomembranous protector

Directory of Open Access Journals (Sweden)

Bijo Mathew

2013-01-01

Full Text Available Purpose: The present paper demonstrates the utility of PASS computer-aided program and makes a clear comparison of predicted and observed pharmacological properties of some novel 5-[(2E-1-(1H-benzimidazol-2-yl-3-substituted phenylprop-2-en-1-ylidene] pyrimidine-2, 4, 6 (1H, 3H, 5H-triones (5a-f. Materials and Methods: The synthesis of the titled derivatives were achieved by the reaction between 2E-1-(1H-benzimidazol-2-yl-3-phenylprop-2-en-1-ones (4a-f and barbituric acid in the presence of catalytic amount of acetic acid medium. All the final structures were assigned on the basis of IR, 1 HNMR and mass spectra analysis. All the newly synthesized compounds were screened for their antiulcer activity in the pylorus-ligated rats. Results: Compounds 5b, 5e and 5c showed a percentage protection of (69.58, 69.56 and 67.17 at a dose of 50 mg/kg b.w. when compared to standard omeprazole (77.37%, 2 mg/kg b.w.. Conclusion: Scanning of stomach specimens using electron microscope revealed that the mice treated with standard and synthetic derivatives had no injury observed in stomach mucosa, which is identical to that of the control animal.

Ring retroreflector system consisting of cube-corner reflectors with special coating

International Nuclear Information System (INIS)

Burmistrov, V B; Sadovnikov, M A; Sokolov, A L; Shargorodskiy, V D

2013-01-01

The ring retroreflector system (RS) consisting of cubecorner reflectors (CCRs) with a special coating of reflecting surfaces, intended for uniaxially Earth-oriented navigation satellites, is considered. The error of distance measurement caused by both the laser pulse delay in the CCR and its spatial position (CCR configuration) is studied. It is shown that the ring RS, formed by the CCR with a double-spot radiation pattern, allows the distance measurement error to be essentially reduced. (nanogradient dielectric coatings and metamaterials)

Design considerations for a digital feedback system to control self-bunching in ion-storage rings

Directory of Open Access Journals (Sweden)

V. Ziemann

2001-04-01

Full Text Available We discuss the feasibility of a digital feedback system to cure self-bunching of the electron-cooled coasting ion beam in ion-storage rings such as CELSIUS [S. Holm, A. Johansson, S. Kullander, and D. Reistad, Phys. Scr. 34, 513–532 (1986]. Such a system is based on a fast digital filter that acts as a tunable artificial wake potential. It may also aid stable operation of accumulator rings for future spallation neutron sources or heavy ion rings used for inertial fusion energy production.

A new systematic calibration method of ring laser gyroscope inertial navigation system

Science.gov (United States)

Wei, Guo; Gao, Chunfeng; Wang, Qi; Wang, Qun; Xiong, Zhenyu; Long, Xingwu

2016-10-01

Inertial navigation system has been the core component of both military and civil navigation systems. Before the INS is put into application, it is supposed to be calibrated in the laboratory in order to compensate repeatability error caused by manufacturing. Discrete calibration method cannot fulfill requirements of high-accurate calibration of the mechanically dithered ring laser gyroscope navigation system with shock absorbers. This paper has analyzed theories of error inspiration and separation in detail and presented a new systematic calibration method for ring laser gyroscope inertial navigation system. Error models and equations of calibrated Inertial Measurement Unit are given. Then proper rotation arrangement orders are depicted in order to establish the linear relationships between the change of velocity errors and calibrated parameter errors. Experiments have been set up to compare the systematic errors calculated by filtering calibration result with those obtained by discrete calibration result. The largest position error and velocity error of filtering calibration result are only 0.18 miles and 0.26m/s compared with 2 miles and 1.46m/s of discrete calibration result. These results have validated the new systematic calibration method and proved its importance for optimal design and accuracy improvement of calibration of mechanically dithered ring laser gyroscope inertial navigation system.

Electronic de-multipliers II (ring-shape systems)

International Nuclear Information System (INIS)

Raievski, V.

1948-09-01

This report describes a new type of ring-shape fast electronic counter (de-multiplier) with a resolution capacity equivalent to the one made by Regener (Rev. of Scientific Instruments USA 1946, 17, 180-89) but requiring two-times less electronic valves. This report follows the general description of electronic de-multipliers made by J. Ailloud (CEA--001). The ring comprises 5 flip-flop circuits with two valves each. The different elements of the ring are calculated with enough details to allow the transfer of this calculation to different valve types. (J.S.)

Data exchange system in cooler-storage-ring virtual accelerator

International Nuclear Information System (INIS)

Liu Wufeng; Qiao Weimin; Jing Lan; Guo Yuhui

2009-01-01

The data exchange system of the cooler-storage-ring (CSR) control system for heavy ion radiotherapy has been introduced for the heavy ion CSR at Lanzhou (HIRFL-CSR). Using techniques of Java, component object model (COM), Oracle, DSP and FPGA, this system can achieve real-time control of magnet power supplies sanctimoniously, and control beams and their switching in 256 energy levels. It has been used in the commissioning of slow extraction for the main CSR (CSRm), showing stable and reliable performance. (authors)

The Centaur Chariklo and its rings system from stellar occultations in 2017

Science.gov (United States)

Leiva, Rodrigo; Sicardy, Bruno; Camargo, Julio; Ortiz, Jose Luis; Berard, Diane; Desmars, Josselin; Chariklo Occultations Team; Rio Group; Lucky Star Occultation Team; Granada Occultation Team

2017-10-01

A stellar occultation in June 3, 2013 revealed the presence of a dense ring system around the Centaur object (10199) Chariklo (Braga-Ribas et al., Nature 2014). Subsequent analysis of occultation data and long-term photometric variations indicate that Chariklo's body is elongated (Leiva et al. 2017, submitted) and that the main ring exhibits significant longitudinal variations of the radial width (Bérard et al. 2017, in press). We report three multi-chord high-quality stellar occultation by Chariklo on April 9, 2017 and June 22, 2017 from Namibia, and July 23 2017 from South America. The analysis of this new data set is underway, but preliminary results are consistent with triaxial ellipsoidal models. From this analysis we will:-present refined models for the size and shape of Chariklo's main body andevaluate the heights and slopes of its topographic features.-give constraints on the longitudinal width variations of Chariklo's rings andexplore the possibility to obtain the rings apsidal precession rate.Chariklo's shape and topography have strong consequences on the dynamics of the rings through Lindblad-type resonances between mean motion of the ring particles and the spin of the main body, while the rings precession rate gives constraints on the dynamical oblateness of the main body.**Part of the research leading to these results has received funding from the European Research Council under the European Community’s H2020 (2014-2020/ ERC Grant Agreement n 669416 ”LUCKY STAR”).

Radio frequency system of the RIKEN ring cyclotron

International Nuclear Information System (INIS)

Fujisawa, T.; Ogiwara, K.; Kohara, S.; Oikawa, Y.; Yokoyama, I.; Nagase, M.; Takeshita, I.; Chiba, Y.; Kumata, Y.

1987-01-01

The radio-frequency(RF) system of the RIKEN ring cyclotron(K = 540) is required to work in a frequency range of 20 to 45 MHz and to generate the maximum acceleration voltage 250 kV. A new movable box type variable frequency resonator was designed for that purpose. The final amplifier is capable to deliver 300 kW. The resonators and the amplifiers have been installed at RIKEN and the performances are studied. The result shows the movable box type resonator and the power amplifier system satisfy the design aim. (author)

Digital closed orbit feedback system for the Advanced Photon Source storage ring

International Nuclear Information System (INIS)

Chung, Y.; Barr, D.; Decker, G.; Galayda, J.; Lenkszus, F.; Lumpkin, A.; Votaw, A.J.

1995-01-01

Closed orbit feedback for the Advanced Photon Source (APS) storage ring employs unified global an local feedback systems for stabilization of particle and photon beams based on digital signal processing (DSP). Hardware and software aspects of the system will be described. In particular, we will discuss global and local orbit feedback algorithms, PID (proportional, integral, and derivative) control algorithm. application of digital signal processing to compensate for vacuum chamber eddy current effects, resolution of the interaction between global and local systems through decoupling, self-correction of the local bump closure error, user interface through the APS control system, and system performance in the frequency and time domains. The system hardware, including the DSPS, is distributed in 20 VNE crates around the ring, and the entire feedback system runs synchronously at 4-kHz sampling frequency in order to achieve a correction bandwidth exceeding 100 Hz. The required data sharing between the global and local feedback systems is facilitated via the use of fiber-optically-networked reflective memories

Aromatic carboxylate effect on dimensionality of three bis(benzimidazole)-based cobalt(II) coordination polymers: Syntheses, structures and properties

International Nuclear Information System (INIS)

Zhang, Ju-Wen; Gong, Chun-Hua; Hou, Li-Li; Tian, Ai-Xiang; Wang, Xiu-Li

2013-01-01

Three new metal-organic coordination polymers [Co(4-bbc) 2 (bbbm)] (1), [Co(3,5-pdc)(bbbm)]·2H 2 O (2) and [Co(1,4-ndc)(bbbm)] (3) (4-Hbbc=4-bromobenzoic acid, 3,5-H 2 pdc=3,5-pyridinedicarboxylic acid, 1,4-H 2 ndc=1,4-naphthalenedicarboxylic acid and bbbm=1,1-(1,4-butanediyl)bis-1H-benzimidazole) were hydrothermally synthesized and structurally characterized. Polymer 1 is a 1D chain formed by the bbbm ligands and Co II ions. Polymer 2 exhibits a 2D network with a (3·4·5)(3 2 ·4·5·6 2 ·7 4 ) topology. Polymer 3 possesses a 3D three-fold interpenetrating framework. The versatile structures of title polymers indicate that the aromatic carboxylates have an important influence on the dimensionality of 1–3. Moreover, the thermal stability, electrochemical and luminescent properties of 1–3 were investigated. - graphical abstract: Three bis(benzimidazole)-based cobalt(II) coordination polymers tuned by aromatic carboxylates were hydrothermally synthesized and structurally characterized. The aromatic carboxylates play a key role in the dimensionality of three polymers. The electrochemical and luminescent properties of three polymers were investigated. Display Omitted - Highlights: • Three bis(benzimidazole)-based cobalt(II) coordination polymers tuned by aromatic carboxylates were obtained. • The aromatic carboxylates have an important influence on the dimensionality of three polymers. • The electrochemical and luminescent properties of three polymers were investigated

Steady state and time-resolved spectroscopic investigations on the photoreactions involved within the electronically excited electron acceptor 9-cyanoanthracene in presence of benzotriazole and benzimidazole donors

International Nuclear Information System (INIS)

Bhattacharya, Sudeshna; Bardhan, Munmun; Ganguly, Tapan

2010-01-01

The electrochemical, 'steady-state' and 'time-resolved' spectroscopic investigations were made on the well-known electron acceptor 9-cyanoanthracene (CNA) when interacted with the electron donors benzotriazole (BZT) and benzimidazole (BMI) molecules. Though electrochemical measurements indicate the thermodynamical possibility of occurrences of photoinduced electron transfer reactions within these reacting systems in the lowest excited singlet state (S 1 ) of the acceptor CNA but the steady-state and time-resolved measurements clearly demonstrate only the triplet-initiated charge separation reactions. It was reported earlier that in the cases of disubstituted indole molecules the occurrences of photoinduced electron transfer reactions were apparent both in the excited singlet and triplet states of the acceptor 9-cyanoanthracene, but the similarly structured present donor molecules benzotriazole (and benzimidazole) behave differently from indoles. The weak ground state complex formations within the presently studied reacting systems appear to be responsible for the observed static quenching phenomena as evidenced from the time-resolved fluorescence studies. Time-resolved spectroscopic investigations demonstrate the formation of the ground state of the reacting components (donor and acceptor) through recombination of triplet ion-pairs via formations of contact neutral radical produced by H-abstraction mechanism.

An Alternative Derivation of the Energy Levels of the "Particle on a Ring" System

Science.gov (United States)

Vincent, Alan

1996-10-01

All acceptable wave functions must be continuous mathematical functions. This criterion limits the acceptable functions for a particle in a linear 1-dimensional box to sine functions. If, however, the linear box is bent round into a ring, acceptable wave functions are those which are continuous at the 'join'. On this model some acceptable linear functions become unacceptable for the ring and some unacceptable cosine functions become acceptable. This approach can be used to produce a straightforward derivation of the energy levels and wave functions of the particle on a ring. These simple wave mechanical systems can be used as models of linear and cyclic delocalised systems such as conjugated hydrocarbons or the benzene ring. The promotion energy of an electron can then be used to calculate the wavelength of absorption of uv light. The simple model gives results of the correct order of magnitude and shows that, as the chain length increases, the uv maximum moves to longer wavelengths, as found experimentally.

Generation of radiation by benzimidazoles in various aggregate states

Energy Technology Data Exchange (ETDEWEB)

Gruzinsky, V V; Degtyarenko, K M; Shalaev, V K; Kopylova, T N; Verkhovsky, V S; Tarasenko, V F; Melochenko, S V

1983-04-01

Lasing has been obtained on the solutions of new derivatives of benzimidazole (Bi): 2-phenyl-Bi (the band maximum lambda/sub r.max/ = 341/347 nm), 2-n-tolyl-Bi (344 nm) and 2-(4'-biphenilyl) Bi (366/374 nm). Compounds of this class provide a perspective basis for laser radiation covering of a wide spectrum region. Lasing has been obtained on the vapors of 2-(4'-biphenilyl)Bi (361.2 nm) and 2-(n-tolyl) Bi (336.3 nm) with pentane stabilizer of excited states. High volatility, photostability and laser-action over wide concentration ranges determine the efficiency of using the new class of compounds - chain arylbenzimitazoles - in lasers based on complex molecule vapors.

In Situ Synthesis of a Magnetic Graphene Platform for the Extraction of Benzimidazoles from Food Samples and Analysis by High-Performance Liquid Chromatography

Directory of Open Access Journals (Sweden)

Qianchun Zhang

2017-01-01

Full Text Available A novel method was proposed for the determination of five benzimidazoles (oxfendazole, mebendazole, flubendazole, albendazole, and fenbendazole using magnetic graphene (G-Fe3O4. G-Fe3O4 was synthesized via in situ chemical coprecipitation. The properties of G-Fe3O4 were characterized by various instrumental methods. G-Fe3O4 exhibited a great adsorption ability and good stability towards analytes. Various experimental parameters that might affect the extraction efficiency such as the amount of G-Fe3O4, extraction solvent, extraction time, and desorption conditions were evaluated. Under the optimized conditions, a method based on G-Fe3O4 magnetic solid-phase extraction coupled with high-performance liquid chromatography was developed. A good linear response was observed in the concentration range of 0.100–100 μg/L for the five benzimidazoles, with correlation coefficients ranging from 0.9966 to 0.9998. The limits of detection (S/N=3 of the method were between 17.2 and 32.3 ng/L. Trace benzimidazoles in chicken, chicken blood, and chicken liver samples were determined and the concentrations of oxfendazole, mebendazole, flubendazole, and fenbendazole in these samples were 13.0–20.2, 1.62–4.64, 1.94–6.42, and 0.292–1.04 ng/g, respectively. The recovery ranged from 83.0% to 115%, and the relative standard deviations were less than 7.9%. The proposed method was sensitive, reliable, and convenient for the analysis of trace benzimidazoles in food samples.

Sulfonated copolyimide membranes derived from a novel diamine monomer with pendant benzimidazole groups for fuel cells

DEFF Research Database (Denmark)

Li, Wei; Guo, Xiaoxia; Aili, David

2015-01-01

. A series of sulfonated copolyimides (SPI) are prepared via random copolymerizatio of 1,4,5,8-naphthalenetetracarboxylic dianhydride (NTDA) with a new diamine monomer with pendant benzimidazole groups, 2,2'-bis(4-(1H-benzo[d]imidazol-2-yl)phenoxy)benzidine (BIPOB), and a sulfonated diamine monomer 4,4'-bis...

A novel sodium iodide and ammonium molybdate co-catalytic system for the efficient synthesis of 2-benzimidazoles using hydrogen peroxide under ultrasound irradiation.

Science.gov (United States)

Bai, Guo-Yi; Lan, Xing-Wang; Chen, Guo-Feng; Liu, Xiao-Fang; Li, Tian-Yu; Shi, Ling-Juan

2014-03-01

The reaction of aldehydes and o-phenylenediamine for the preparation of 2-benzimidazoles has been studied using hydrogen peroxide as an oxidant under ultrasound irradiation at room temperature in this paper. The combination of substoichiometric sodium iodide and ammonium molybdate as co-catalysts, together with using small amounts of hydrogen peroxide, makes this transformation very efficient and attractive under ultrasound. Thus, a mild, green and efficient method is established to carry out this reaction in high yield. Copyright © 2013 Elsevier B.V. All rights reserved.

The kicker magnet system for TRISTAN Accumulation Ring injection

International Nuclear Information System (INIS)

Sakamoto, Y.; Satoh, K.; Nakayama, H.

1994-12-01

The injection of electron beams to TRISTAN Accumulation Ring (AR) was started in November 1983 and the positron injection started in November 1985. For the injection of electron and positron beams to AR, the unique kicker system was developed. In the kicker power supply the charging to the main capacitor was done with the resonant charge system together with the auxiliary charging unit. The impedance matching circuit was added to the kicker magnet for getting the required current form with least reflecting oscillation. In this paper we report the performance of this kicker system. (author)

The Synthesis and Biological Evaluation of N-Substituted 1H-Benzimidazol-2-yl-1H-pyrazole-3,5-diamines

Czech Academy of Sciences Publication Activity Database

Jedinák, L.; Kryštof, Vladimír; Cankař, P.

2016-01-01

Roč. 53, č. 2 (2016), s. 499-507 ISSN 0022-152X Institutional support: RVO:61389030 Keywords : ONE-POT SYNTHESIS * BENZIMIDAZOLE DERIVATIVES * EFFICIENT SYNTHESIS Subject RIV: CE - Biochemistry Impact factor: 0.893, year: 2016

Synthesis of novel tripodal-benzimidazole from 2,4,6-tris(p-formylphenoxy)-1,3,5-triazine: Structural, electrochemical and antimicrobial studies

International Nuclear Information System (INIS)

Koc, Ziya Erdem; Bingol, Haluk; Saf, Ahmet O.; Torlak, Emrah; Coskun, Ahmet

2010-01-01

Four new tripodal-benzimidazole derivatives were synthesized by Schiff base reaction between 2,4,6-tris(p-formylphenoxy)-1,3,5-triazine (TRIPOD) and different diamine derivatives. The structures of the obtained compounds were identified by FT-IR, 1 H NMR, 13 C NMR and UV-vis spectral data, thermal analysis and elemental analysis. Electrochemical behaviors of the compounds were studied by cyclic voltammetry in DMF including 0.1 M [NBu 4 ] [PF 6 ]. The voltammograms showed peaks having similar characteristics except tripodal-benzimidazole including -NO 2 derivative. In addition, their antimicrobial activities were evaluated by using the standard disk diffusion method in dimethylformamide media. The activities were determined against 4 bacteria cultures by comparing to those of gentamycin.

Synthesis, DNA binding ability and anticancer activity of 2-heteroaryl substituted benzimidazoles linked pyrrolo[2,1-c][1,4]benzodiazepine conjugates.

Science.gov (United States)

Kamal, Ahmed; Pogula, Praveen Kumar; Khan, Mohammed Naseer Ahmed; Seshadri, Bobburi Naga; Sreekanth, Kokkonda

2013-08-01

As a continuation of our efforts to develop the benzimidazole-PBD conjugates as potential anticancer agents, a series of heteroaryl substituted benzimidazole linked PBD conjugates has been synthesized and evaluated for their anticancer potential in 60 human cancer cell lines. Most of the compounds exhibited promising anticancer activity and interestingly, compounds 4c and 4d displayed significant activity in most of the cell lines tested. Whereas, compound 4e showed selectivity in renal cancer cells with GI50 values of <10 and 70 nM against RXF 393 and UO-31 cell lines, respectively. Further, these compounds also showed significant DNA-binding affinity by thermal denaturation study using duplex form of calf thymus (CT) DNA.

SULFONATED POLY(ARYLENE ETHER BENZIMIDAZOLE COPOLYMER MEMBRANE SYNTHESIS AND CHARACTERIZATION

Directory of Open Access Journals (Sweden)

Çağla TOSUN

2015-05-01

Full Text Available Hidrojenden elektrik enerjisi üretiminde kullanılan yakıt hücreleri, geleceğin çevre dostu ve yüksek verimli enerji üretimine alternatif olarak kabul görmektedirler. Nafion gibi perflorosülfonik asit bazlı membranlar polimer elektrolit membran yakıt hücreleri (PEMHY’nde sıklıkla kullanılmaktadırlar. Ancak Nafion membranların yüksek sıcaklıklarda proton iletkenliklerinin düşmesi ve fiyatlarının yüksek olması nedeniyle alternatif polimer elektrolit membran (PEM’lar üzerine araştırmalar devam etmektedir. Bu çalışmanın ilk aşamasında, disodyum-3,3’-disülfonat-4,4’-diklorodifenilsülfon (SDCDPS ve benzimidazol bisfenol (HPBI monomerlerinin sentezi gerçekleştirilmiştir. Daha sonra sentezlenen monomerlerden nükleofilik aromatik polikondenzasyon reaksiyonu ile poli(arilen eter benzimidazol kopolimeri sentezlenmiştir. Sentezlenen monomerlerin 1H NMR ve FTIR, kopolimerin ise 1H NMR, FTIR ve termogravimetrik analizleri (TGA gerçekleştirilmiştir. Yapılan analizler sonucunda kopolimerin sentezlendiği açıkça ortaya konulmuştur. TGA eğrisi sentezlenen kopolimerin ısıl kararlılığının yüksek olduğunu (~400 oC ve yüksek sıcaklık uygulamalarında kullanılabilirliğini göstermiştir

Systematic Search for Rings around Kepler Planet Candidates: Constraints on Ring Size and Occurrence Rate

Science.gov (United States)

Aizawa, Masataka; Masuda, Kento; Kawahara, Hajime; Suto, Yasushi

2018-05-01

We perform a systematic search for rings around 168 Kepler planet candidates with sufficient signal-to-noise ratios that are selected from all of the short-cadence data. We fit ringed and ringless models to their light curves and compare the fitting results to search for the signatures of planetary rings. First, we identify 29 tentative systems, for which the ringed models exhibit statistically significant improvement over the ringless models. The light curves of those systems are individually examined, but we are not able to identify any candidate that indicates evidence for rings. In turn, we find several mechanisms of false positives that would produce ringlike signals, and the null detection enables us to place upper limits on the size of the rings. Furthermore, assuming the tidal alignment between axes of the planetary rings and orbits, we conclude that the occurrence rate of rings larger than twice the planetary radius is less than 15%. Even though the majority of our targets are short-period planets, our null detection provides statistical and quantitative constraints on largely uncertain theoretical models of the origin, formation, and evolution of planetary rings.

Simulation of Small Wind Turbine Generation System Using Ring Winding Slotless PMSG by FEM

OpenAIRE

徳永, 翔平; 袈裟丸, 勝己; Tokunaga, Shohei; Kesamaru, Katsumi

2011-01-01

This paper describes a novel small wind turbine generation system with ring winding slotless PMSG. To reduce cogging torque, ring winding PM generator is used for a wind turbine generator. Using finite element analysis, the characteristics of slotless PMSGs are elucidated and the dynamic performance of the proposed system with MPPT control is represented. In this paper, the constant wind test and the quasi-natural wind test are conducted. The results of these tests indicate the proposed syste...

Pressure injection of methyl 2-benzimidazole carbamate hydrochloride solution as a control for Dutch elm disease

Science.gov (United States)

Garold F. Gregory; Thomas W. Jones

1973-01-01

A preliminary evaluation of the effectiveness of injecting methyl 2-benzimidazole carbamate hydrochloride solution into elms for prevention or cure of Dutch elm disease is reported. Symptom development was diminished or prevented in elms injected with fungicide before inoculation. Symptom development was arrested in all crown-inoculated diseased trees injected with the...

Synthesis of amino ester-embedded benzimidazoles: a one-pot sequential protocol under metal-free neutral conditions.

Science.gov (United States)

Roy, Priyabrata; Bodhak, Chandan; Pramanik, Animesh

2017-02-01

A one-pot three-component protocol has been developed for the synthesis of amino ester-embedded benzimidazoles under metal-free neutral conditions. Sequentially, the methodology involves coupling of an amino ester with 1-fluoro-2-nitrobenzene, reduction of the coupled nitroarene by sodium dithionite, and cyclization of the corresponding diamine with an aldehyde.

Design, synthesis and biological evaluation of 5-fluorouracil-derived benzimidazoles as novel type of potential antimicrobial agents.

Science.gov (United States)

Fang, Xue-Jie; Jeyakkumar, Ponmani; Avula, Srinivasa Rao; Zhou, Qian; Zhou, Cheng-He

2016-06-01

A series of 5-fluorouracil benzimidazoles as novel type of potential antimicrobial agents were designed and synthesized for the first time. Bioactive assay manifested that some of the prepared compounds exhibited good or even stronger antibacterial and antifungal activities against the tested strains in comparison with reference drugs norfloxacin, chloromycin and fluconazole. Noticeably, 3-fluorobenzyl benzimidazole derivative 5c gave remarkable antimicrobial activities against Saccharomyces cerevisiae, MRSA and Bacillus proteus with MIC values of 1, 2 and 4μg/mL, respectively. Experimental research revealed that compound 5c could effectively intercalate into calf thymus DNA to form compound 5c-DNA complex which might block DNA replication and thus exert antimicrobial activities. Molecular docking indicated that compound 5c should bind with DNA topoisomerase IA through three hydrogen bonds by the use of fluorine atom and oxygen atoms in 5-fluorouracil with the residue Lys 423. Copyright © 2016 Elsevier Ltd. All rights reserved.

Design, synthesis and evaluation of novel 2,5,6-trisubstituted benzimidazoles targeting FtsZ as antitubercular agents.

Science.gov (United States)

Park, Bora; Awasthi, Divya; Chowdhury, Soumya R; Melief, Eduard H; Kumar, Kunal; Knudson, Susan E; Slayden, Richard A; Ojima, Iwao

2014-05-01

Filamenting temperature-sensitive protein Z (FtsZ), an essential cell division protein, is a promising target for the drug discovery of new-generation antibacterial agents against various bacterial pathogens. As a part of SAR studies on benzimidazoles, we have synthesized a library of 376 novel 2,5,6-trisubstituted benzimidazoles, bearing ether or thioether linkage at the 6-position. In a preliminary HTP screening against Mtb H37Rv, 108 compounds were identified as hits at a cut off concentration of 5 μg/mL. Among those hits, 10 compounds exhibited MIC values in the range of 0.63-12.5 μg/mL. Light scattering assay and TEM analysis with the most potent compound 5a clearly indicate that its molecular target is Mtb-FtsZ. Also, the Kd of 5a with Mtb-FtsZ was determined to be 1.32 μM. Copyright © 2014 Elsevier Ltd. All rights reserved.

Simulation of the control system for the KEK main ring power supply-II

International Nuclear Information System (INIS)

Kabe, Atsushi; Sato, Hikaru; Masuda, Masayoshi; Takeda, Masahiro; Nakano, Michio

1977-05-01

The tracking error between the magnetic field of the bending magnets and that of the quadrupole magnets is a very important problem of the KEK main ring power supply. Tacking performance is simulated using DDS (Digital Dynamics Simulator) in cases of 8 GeV and 12 GeV operation of the KEK main ring. The results of simulation coincide with the data of actual system. (auth.)

Cryogenic systems for large superconducting accelerators/storage rings

International Nuclear Information System (INIS)

Brown, D.P.

1981-01-01

Particle accelerators and storage rings which utilize superconducting magnets have presented cryogenic system designers, as well as magnet designers, with many new challenges. When such accelerators were first proposed, little operational experience existed to guide the design. Two superconducting accelerators, complete with cryogenic systems, have been designed and are now under construction. These are the Fermilab Doubler Project and the Brookhaven National Laboratory ISABELLE Project. The cryogenic systems which developed at these two laboratories share many common characteristics, especially as compared to earlier cryogenic systems. Because of this commonality, these characteristics can be reasonably taken as also being representative of future systems. There are other areas in which the two systems are dissimilar. In those areas, it is not possible to state which, if either, will be chosen by future designers. Some of the design parameters for the two systems are given

Topological ring currents in the "empty" ring of benzo-annelated perylenes.

Science.gov (United States)

Dickens, Timothy K; Mallion, Roger B

2011-01-27

Cyclic conjugation in benzo-annelated perylenes is examined by means of the topological π-electron ring currents calculated for each of their constituent rings, in a study that is an exact analogy of a recent investigation by Gutman et al. based on energy-effect values for the corresponding rings in each of these structures. "Classical" approaches, such as Kekulé structures, Clar "sextet" formulas, and circuits of conjugation, predict that the central ring in perylene is "empty" and thus contributes negligibly to cyclic conjugation. However, conclusions from the present calculations of topological ring currents agree remarkably with those arising from the earlier study involving energy-effect values in that, contrary to what would be predicted from the classical approaches, rings annelated in an angular fashion relative to the central ring of these perylene structures materially increase the extent of that ring's involvement in cyclic conjugation. It is suggested that such close quantitative agreement between the predictions of these two superficially very different indices (energy effect and topological ring current) might be due to the fact that, ultimately, both depend, albeit in ostensibly quite different ways, only on an adjacency matrix that contains information about the carbon-carbon connectivity of the conjugated system in question.

An analog RF gap voltage regulation system for the Advanced Photon Source storage ring

International Nuclear Information System (INIS)

Horan, D.

1999-01-01

An analog rf gap voltage regulation system has been designed and built at Argonne National Laboratory to maintain constant total storage ring rf gap voltage, independent of beam loading and cavity tuning effects. The design uses feedback control of the klystron mod-anode voltage to vary the amount of rf power fed to the storage ring cavities. The system consists of two independent feedback loops, each regulating the combined rf gap voltages of eight storage ring cavities by varying the output power of either one or two rf stations, depending on the mode of operation. It provides full operator control and permissive logic to permit feedback control of the rf system output power only if proper conditions are met. The feedback system uses envelope-detected cavity field probe outputs as the feedback signal. Two different methods of combining the individual field probe signals were used to generate a relative DC level representing one-half of the total storage ring rf voltage, an envelope-detected vector sum of the field probe rf signals, and the DC sum of individual field probe envelope detector outputs. The merits of both methods are discussed. The klystron high-voltage power supply (HVPS) units are fitted with an analog interface for external control of the mod-anode voltage level, using a four-quadrant analog multiplier to modulate the HVPS mod-anode voltage regulator set-point in response to feedback system commands

PF-KO system for single bunch mode operation of a storage ring

International Nuclear Information System (INIS)

Ohgaki, H.; Sugiyama, S.; Mikado, T.; Chiwaki, M.; Yamada, K.; Suzuki, R.; Sei, N.; Noguchi, T.; Yamazaki, T.

1994-01-01

A new RF-KO (RF knockout) system for the single bunch mode operation of a storage ring has been developed. The knockout signal is modulated by the sum signal of the RF acceleration frequency of the storage ring and a bunch selection signal. We do not need any special device or a timing unit with this method. We obtain a high purity of bunch structure in a short knock out time. The single bunch impurity of 0.2% has been achieved. (author)

Nonlinear analysis of ring oscillator circuits

KAUST Repository

Ge, Xiaoqing

2010-06-01

Using nonlinear systems techniques, we analyze the stability properties and synchronization conditions for ring oscillator circuits, which are essential building blocks in digital systems. By making use of its cyclic structure, we investigate local and global stability properties of an n-stage ring oscillator. We present a sufficient condition for global asymptotic stability of the origin and obtain necessity if the ring oscillator consists of identical inverter elements. We then give a synchronization condition for identical interconnected ring oscillators.

Nonlinear analysis of ring oscillator circuits

KAUST Repository

Ge, Xiaoqing; Arcak, Murat; Salama, Khaled N.

2010-01-01

Using nonlinear systems techniques, we analyze the stability properties and synchronization conditions for ring oscillator circuits, which are essential building blocks in digital systems. By making use of its cyclic structure, we investigate local and global stability properties of an n-stage ring oscillator. We present a sufficient condition for global asymptotic stability of the origin and obtain necessity if the ring oscillator consists of identical inverter elements. We then give a synchronization condition for identical interconnected ring oscillators.

Preparation of stir cake sorptive extraction based on polymeric ionic liquid for the enrichment of benzimidazole anthelmintics in water, honey and milk samples

Energy Technology Data Exchange (ETDEWEB)

Wang, Yulei [State Key Laboratory of Marine Environmental Science, Key Laboratory of the Ministry of Education for Coastal and Wetland Ecosystem, College of the Environment and Ecology, Xiamen University, Siming Road, P.O. Box 1009, Xiamen 361005 (China); Zhang, Jie [Key Lab of Urban Environment and Health, Institute of Urban Environment, Chinese Academy of Sciences (China); Huang, Xiaojia, E-mail: hxj@xmu.edu.cn [State Key Laboratory of Marine Environmental Science, Key Laboratory of the Ministry of Education for Coastal and Wetland Ecosystem, College of the Environment and Ecology, Xiamen University, Siming Road, P.O. Box 1009, Xiamen 361005 (China); Yuan, Dongxing [State Key Laboratory of Marine Environmental Science, Key Laboratory of the Ministry of Education for Coastal and Wetland Ecosystem, College of the Environment and Ecology, Xiamen University, Siming Road, P.O. Box 1009, Xiamen 361005 (China)

2014-08-20

Highlights: • A new polymeric ionic liquid-based monolith was prepared. • The monolith was used as the extractive medium of stir cake sorptive extraction. • The SCSE–AMIIDB can extract benzimidazole anthelmintics (BAs) effectively. • A combination of SCSE–AMIIDB–LD–HPLC/DAD was developed. • The combination was applied to monitor trace BAs in water, milk and honey samples. - Abstract: In this work, a new stir cake sorptive extraction (SCSE) using polymeric ionic liquid monolith as sorbent was prepared. The sorbent was obtained by in situ copolymerization of an ionic liquid, 1-allyl-3-methylimidazolium bis[(trifluoro methyl)sulfonyl]imide (AMII) and divinylbenzene (DB) in the presence of N,N-dimethylformamide. The influence of the content of ionic liquid and the porogen in the polymerization mixture on extraction performance was studied thoroughly. The physicochemical properties of the polymeric ionic liquid were characterized by infrared spectroscopy, elemental analysis, scanning electron microscopy and mercury intrusion porosimetry. The usefulness of SCSE–AMIIDB was demonstrated by the enrichment of trace benzimidazole anthelmintics. Several parameters affecting the extraction efficiency were investigated, and under the optimized conditions, a simple and effective method for the determination of trace benzimidazoles residues in water, milk and honey samples was established by coupling SCSE–AMIIDB with high performance liquid chromatography/diode array detection (SCSE–AMIIDB–HPLC/DAD). Results indicated that the limits of detection (S/N = 3) for target compounds were 0.020–0.072 μg L{sup −1}, 0.035–0.10 μg L{sup −1} and 0.026–0.076 μg L{sup −1} in water, milk and honey samples, respectively. In addition, an acceptable reproducibility was achieved by evaluating the repeatability and intermediate precision with relative standard deviations (RSD) of less than 9% and 11%, respectively. Finally, the established AMII�

Virus-directed enzyme prodrug therapy and the assessment of the cytotoxic impact of some benzimidazole derivatives.

Science.gov (United States)

Szewczuk, Michał; Boguszewska, Karolina; Żebrowska, Marta; Balcerczak, Ewa; Stasiak, Marta; Świątkowska, Maria; Błaszczak-Świątkiewicz, Katarzyna

2017-07-01

Virus-directed enzyme prodrug therapy is one of the major strategy of increasing cytotoxicity of bioreductive agents. This research intended to examine new selected benzimidazole derivatives as a substrate for nitroreductase, the enzyme involved in nitroreduction which is responsible to the production of cytotoxic metabolites. In this way, the selectivity and strength of cytotoxicity can be raised. The effect of benzimidazoles on virus transfected cells and non-virus transfected cells A549 cell line was established by Annexin V + propidium iodide test, western blot, and polymerase chain reaction analysis of specific pro- and anti-apoptotic proteins in the corresponding gene expression and additionally nitroreductase gene expression. Our results proved the pro-apoptotic properties of all tested compounds in normoxia and hypoxia, especially according to virused A549 cells where the time of exposition was reduced from 48 to 4 h. In this shorten period of time, the strongest activity was shown by N-oxide compounds with nitro-groups. The apoptosis was confirmed by generation of BAX gene and protein and reduction of BCL2 gene and protein.

Variable diameter CO2 laser ring-cutting system adapted to a zoom microscope for applications on polymer tapes.

Science.gov (United States)

Förster, Erik; Bohnert, Patrick; Kraus, Matthias; Kilper, Roland; Müller, Ute; Buchmann, Martin; Brunner, Robert

2016-11-20

This paper presents the conception and implementation of a variable diameter ring-cutting system for a CO2 laser with a working wavelength of 10.6 μm. The laser-cutting system is adapted to an observation zoom microscope for combined use and is applicable for the extraction of small circular areas from polymer films, such as forensic adhesive tapes in a single shot. As an important characteristic for our application, the variable diameter ring-cutting system provides telecentricity in the target area. Ring diameters are continuously tunable between 500 μm and 2 mm. A minimum width of less than 20 μm was found for the ring profile edge. The basic characteristics of the system, including telecentricity, were experimentally evaluated and demonstrated by cutting experiments on different polymer tapes and further exemplary samples.

Synthesis of novel synthetic intermediates from the reaction of benzimidazole and triazole carbenes with ketenimines and their application in the construction of spiro-pyrroles.

Science.gov (United States)

Mo, Jun-Ming; Ma, Yang-Guang; Cheng, Ying

2009-12-07

2-(2-Alkoxycarbonyl-1-arylamino-1-propenyl)benzimidazolium and 5-(2-alkoxycarbonyl-1-arylamino-1-propenyl)triazolium salts were synthesized in good yields from the reaction of benzimidazole and triazole carbenes with ketenimines. Upon treatment with a base, both salts were converted into novel 1,3-dipoles which underwent [3+2] cycloaddition reactions with electron-deficient alkynes and allenes to produce benzimidazole-spiro-pyrroles or triazole-spiro-pyrroles. This work provides novel synthons for the construction of multifunctional spiro-pyrrole derivatives that are not easy accessible by other synthetic methods and are potentially amenable to further transformations.

Design, Synthesis and Biological Evaluation of 2-(2-Amino-5(6-nitro-1H-benzimidazol-1-yl-N-arylacetamides as Antiprotozoal Agents

Directory of Open Access Journals (Sweden)

Emanuel Hernández-Núñez

2017-04-01

Full Text Available Parasitic diseases are a public health problem affecting millions of people worldwide. One of the scaffolds used in several drugs for the treatment of parasitic diseases is the benzimidazole moiety, a heterocyclic aromatic compound. This compound is a crucial pharmacophore group and is considered a privileged structure in medicinal chemistry. In this study, the benzimidazole core served as a model for the synthesis of a series of 2-(2-amino-5(6-nitro-1H-benzimidazol-1-yl-N-arylacetamides 1–8 as benznidazole analogues. The in silico pharmacological results calculated with PASS platform exhibited chemical structures highly similar to known antiprotozoal drugs. Compounds 1–8 when evaluated in silico for acute toxicity by oral dosing, were less toxic than benznidazole. The synthesis of compounds 1–8 were carried out through reaction of 5(6-nitro-1H-benzimidazol-2-amine (12 with 2-chlroactemides 10a–h, in the presence of K2CO3 and acetonitrile as solvent, showing an inseparable mixture of two regioisomers with the -NO2 group in position 5 or 6 with chemical yields of 60 to 94%. The prediction of the NMR spectra of molecule 1 coincided with the experimental chemical displacements of the regioisomers. Comparisons between the NMR prediction and the experimental data revealed that the regioisomer endo-1,6-NO2 predominated in the reaction. The in vitro antiparasitic activity of these compounds on intestinal unicellular parasites (Giardia intestinalis and Entamoeba histolytica and a urogenital tract parasite (Trichomonas vaginalis were tested. Compound 7 showed an IC50 of 3.95 μM and was 7 time more active against G. intestinalis than benznidazole. Compounds 7 and 8 showed 4 times more activity against T. vaginalis compared with benznidazole.

A Study of Storage Ring Requirements for an Explosive Detection System Using NRA Method

CERN Document Server

Wang, Tai-Sen

2005-01-01

The technical feasibility of an explosives detection system based on the nuclear resonance absorption (NRA) of gamma rays in nitrogen-rich materials was demonstrated at Los Alamos National Laboratory (LANL) in 1993 by using an RFQ proton accelerator and a tomographic imaging prototype.* The study is being continued recently to examine deployment of such an active interrogation system in realistic scenarios. The approach is to use a cyclotron and electron-cooling-equipped storage rings(s) to provide the high quality and high current proton beam needed in a practical application. In this work, we investigate the storage ring requirements for a variant of the airport luggage inspection system considered in the earlier LANL experiments. Estimations are carried out based on the required inspection throughput, the gamma ray yield, the proton beam emittance growth due to scattering with the photon-production target, beam current limit in the storage ring, and the electron cooling rate. Studies using scaling and reas...

Vibration characteristics of two-stage planetary transmission system with thin-walled ring gear on elastic supports

Science.gov (United States)

Li, JianYing; Hu, QingChun; Zong, ChangFu; Zhu, TianJun; Zhang, ZeXing

2018-03-01

A dual-clutch and dual-speed planetary gears mechanism of a hybrid car coupled-system is taken as research subject, in which the ring gear of planet set II is a thin-walled structure and the clutch friction plates of planet set II are used as its elastic supports. Based on the lumped parameter-rigid elastic coupled dynamic model of two-stage planetary transmission system with thin-walled ring gear on elastic supports, the motion differential equations are established and the dynamic responses are solved by the Runge-Kutta method considering each stage internal and external time-varying mesh stiffness. The vibration displacements of each stage ring gear have been affected differently in time-domain, the translational vibration displacement of the ring gear of planet set I are obviously more than the torsional vibration displacement, but it is opposite for the ring gear of planet set II; The translational and torsional vibration responses of each stage ring gear arrive the peak in low-frequency. The analysis results of this paper can enrich the theoretical research of multistage planetary transmission and provide guidance for dynamic design.

Synthesis of (benzimidazol-2-yl)aniline derivatives as glycogen phosphorylase inhibitors.

Science.gov (United States)

Galal, Shadia A; Khattab, Muhammad; Andreadaki, Fotini; Chrysina, Evangelia D; Praly, Jean-Pierre; Ragab, Fatma A F; El Diwani, Hoda I

2016-11-01

A series of (benzimidazol-2-yl)-aniline (1) derivatives has been synthesized and evaluated as glycogen phosphorylase (GP) inhibitors. Kinetics studies revealed that compounds displaying a lateral heterocyclic residue with several heteroatoms (series 3 and 5) exhibited modest inhibitory properties with IC 50 values in the 400-600μM range. Arylsulfonyl derivatives 7 (Ar: phenyl) and 9 (Ar: o-nitrophenyl) of 1 exhibited the highest activity (series 2) among the studied compounds (IC 50 324μM and 357μM, respectively) with stronger effect than the p-tolyl analogue 8. Copyright © 2016 Elsevier Ltd. All rights reserved.

Electro-optical hybrid slip ring

Science.gov (United States)

Hong, En

2005-11-01

The slip ring is a rotary electrical interface, collector, swivel or rotary joint. It is a physical system that can perform continuous data transfer and data exchange between a stationary and a rotating structure. A slip ring is generally used to transfer data or power from an unrestrained, continuously rotating electro-mechanical system in real-time, thereby simplifying operations and eliminating damage-prone wires dangling from moving joints. Slip rings are widely used for testing, evaluating, developing and improving various technical equipment and facilities with rotating parts. They are widely used in industry, especially in manufacturing industries employing turbo machinery, as in aviation, shipbuilding, aerospace, defense, and in precise facilities having rotating parts such as medical Computerized Tomography (CT) and MRI scanners and so forth. Therefore, any improvement in slip ring technology can impact large markets. Research and development in this field will have broad prospects long into the future. The goal in developing the current slip ring technology is to improve and increase the reliability, stability, anti-interference, and high data fidelity between rotating and stationary structures. Up to now, there have been numerous approaches used for signal and data transfer utilizing a slip ring such as metal contacts, wires, radio transmission, and even liquid media. However, all suffer from drawbacks such as data transfer speed limitations, reliability, stability, electro-magnetic interference and durability. The purpose of the current research is to break through these basic limitations using an optical solution, thereby improving performance in current slip ring applications. This dissertation introduces a novel Electro-Optical Hybrid Slip Ring technology, which makes "through the air" digital-optical communication between stationary and rotating systems a reality with high data transfer speed, better reliability and low interference susceptibility

Tunable optical analog to electromagnetically induced transparency in graphene-ring resonators system.

Science.gov (United States)

Wang, Yonghua; Xue, Chenyang; Zhang, Zengxing; Zheng, Hua; Zhang, Wendong; Yan, Shubin

2016-12-12

The analogue of electromagnetically induced transparency in optical ways has shown great potential in optical delay and quantum-information technology due to its flexible design and easy implementation. The chief drawback for these devices is the bad tunability. Here we demonstrate a tunable optical transparency system formed by graphene-silicon microrings which could control the transparent window by electro-optical means. The device consists of cascaded coupled ring resonators and a graphene/graphene capacitor which integrated on one of the rings. By tuning the Fermi level of the graphene sheets, we can modulate the round-trip ring loss so that the transparency window can be dynamically tuned. The results provide a new method for the manipulation and transmission of light in highly integrated optical circuits and quantum information storage devices.

Los Alamos Proton Storage Ring (PSR) injection deflector system

International Nuclear Information System (INIS)

Jason, A.j.; Higgins, E.F.; Koelle, A.R.

1983-01-01

We describe a pulsed magnetic deflector system planned for the injection system of the PSR. Two sets of magnets, appropriately placed in the optical systems of both the ring and the injection transport line, provide control of the rate at which particles are injected into a given portion of transverse phase space and limit the interaction of stored beam with the injection stripping foil. High-current modulators that produce relatively complex waveforms are required for this purpose. Solid-state drivers using direct feedback to produce the necessary waveforms are discussed as replacements for the more conventional high-voltage tube technology

Synthesis of novel tripodal-benzimidazole from 2,4,6-tris(p-formylphenoxy)-1,3,5-triazine: Structural, electrochemical and antimicrobial studies

Energy Technology Data Exchange (ETDEWEB)

Koc, Ziya Erdem, E-mail: zerdemkoc@gmail.com [Department of Chemistry, Faculty of Science, Selcuk University, 42031 Konya (Turkey); Bingol, Haluk; Saf, Ahmet O. [Department of Chemistry, Faculty of Science, Selcuk University, 42031 Konya (Turkey); Torlak, Emrah [Provincial Control Laboratory, Konya (Turkey); Coskun, Ahmet [Department of Chemistry, Faculty of Science, Selcuk University, 42031 Konya (Turkey)

2010-11-15

Four new tripodal-benzimidazole derivatives were synthesized by Schiff base reaction between 2,4,6-tris(p-formylphenoxy)-1,3,5-triazine (TRIPOD) and different diamine derivatives. The structures of the obtained compounds were identified by FT-IR, {sup 1}H NMR, {sup 13}C NMR and UV-vis spectral data, thermal analysis and elemental analysis. Electrochemical behaviors of the compounds were studied by cyclic voltammetry in DMF including 0.1 M [NBu{sub 4}] [PF{sub 6}]. The voltammograms showed peaks having similar characteristics except tripodal-benzimidazole including -NO{sub 2} derivative. In addition, their antimicrobial activities were evaluated by using the standard disk diffusion method in dimethylformamide media. The activities were determined against 4 bacteria cultures by comparing to those of gentamycin.

An efficient solvent-free synthesis of imidazolines and benzimidazoles using K 4[Fe(CN 6] catalysis

Directory of Open Access Journals (Sweden)

Kabeer A. Shaikh

2012-01-01

Full Text Available Imidazolines and Benzimidazoles have been efficiently synthesized in high yields by treatment of 1,2-diamine with aldehydes using the metal co-ordinate complex K 4[Fe(CN 6] as a catalysis. The method was carried out under solvent free condition via oxidation of carbon-nitrogen bond. The process is green, mild and inexpensive.

Sorption-desorption characteristics of benzimidazole based fungicide 2-(4-fluorophenyl)-1h-benzimidazole on physicochemical properties of selected pakistani soils

International Nuclear Information System (INIS)

Ahmad, K.S.

2014-01-01

A batch equilibrium method has been utilized to investigate the sorption-desorption behavior of a versatile cost-effective fungicide2-(4-fluorophenyl)-1H-benzimidazole) FBNZ on four Pakistani soils geographically distant, from hilly to desert areas. FBNZ is a newly synthesized fungicide prepared in the laboratory and is cost effective than the commercially available fungicides. The adsorption and desorption data were fitted to the Freundlich equation, with values of na = 1, which points to a C-type isotherm. Sorption increases with soil organic carbon content, with greater degree of adsorption for hilly soil and least adsorption on sandy soil of Multan, Punjab. Desorption studies reveal that the adsorbed fungicide are firmly retained by soil particles and present a certain degree of irreversibility. The results indicate that the soil organic matters followed by clay content are the most important soil properties governing the fungicide sorption capacity. (author)

Modelling a Java Ring based implementation of an N-Count payment system

NARCIS (Netherlands)

Revill, J.D.; Hartel, Pieter H.

N-Count is a system for offline value transfer. A prototype of an N-Count payment system has been designed, and it has been implemented in Java. We have used the Java Ring with the Java Card API as a secure device. The system has also been modelled using the Spin model checker. The combined

Vacuum system for the NIJI-III compact storage ring

International Nuclear Information System (INIS)

Miura, F.; Tsutsui, Y.; Takada, H.

1990-01-01

The NIJI-III is a compact storage ring measuring about 15 m in circumference with four superconducting bending magnets. It is under development as a synchrotron light source for X-ray lithography with a stored beam current of 200 mA at a stored beam current of 200 mA at a stored energy level of 615 MeV. The vacuum system is designed to attain a pressure of less than 1 x 10 -9 Torr at beam storage. The compact ring design makes it difficult to install a large number of pumps able to satisfy the required pumping speed. For the purpose of realizing a high pumping speed, a cryopump as a result of cooling the superconducting magnet duct wall to the liquid helium (LHe) temperature is adopted, as a result the total pumping speed to 2.8 x 10 4 l/s is obtained. (author)

Token ring technology report

CERN Document Server

2013-01-01

Please note this is a Short Discount publication. This report provides an overview of the IBM Token-Ring technology and products built by IBM and compatible vendors. It consists of two sections: 1. A summary of the design trade-offs for the IBM Token-Ring. 2. A summary of the products of the major token-ring compatible vendors broken down by adapters and components, wiring systems, testing, and new chip technology.

Self-gravitation in Saturn's rings

International Nuclear Information System (INIS)

Salo, H.; Lukkari, J.

1982-01-01

In a ring-shaped collisional system self-gravitation reduces the equilibrium values of the geometric and optical thickness. In Saturn's rings both effects are appreciable. The previously found discrepancy between the calculated profile and the observed profile of the rings is chiefly caused by the omission of self-gravitation. (Auth.)

Digital closed orbit feedback system for the advanced photon source storage ring

International Nuclear Information System (INIS)

Chung, Y.; Barr, D.; Decker, G.

1995-01-01

The Advanced Photon Source (APS) is a dedicated third-generation synchrotron light source with a nominal energy of 7 GeV and a circumference of 1104 m. The closed orbit feedback system for the APS storage ring employs unified global and local feedback systems for stabilization of particle and photon beams based on digital signal processing (DSP). Hardware and software aspects of the system will be described in this paper. In particular, we will discuss global and local orbit feedback algorithms, PID (proportional, integral, and derivative) control algorithm, application of digital signal processing to compensate for vacuum chamber eddy current effects, resolution of the interaction between global and local systems through decoupling, self-correction of the local bump closure error, user interface through the APS control system, and system performance in the frequency and time domains. The system hardware including the DSPs is distributed in 20 VME crates around the ring, and the entire feedback system runs synchronously at 4-kHz sampling frequency in order to achieve a correction bandwidth exceeding 100 Hz. The required data sharing between the global and local feedback systems is facilitated via the use of fiber-optically-networked reflective memories

Inhibition of partially purified K+/H+-ATPase from guinea-pig isolated and enriched parietal cells by substituted benzimidazoles.

Science.gov (United States)

Beil, W.; Sewing, K. F.

1984-01-01

The cellular and subcellular distributions of adenosinetriphosphatases (ATPases) were examined in guinea-pig gastric mucosal cells. All cell types displayed Mg2+-ATPase and bicarbonate (HCO3-)-stimulated ATPase activity. K+-ATPase was located only in fractions derived from parietal cells. Differential and density-gradient centrifugation of material prepared from parietal cells revealed that K+-ATPase activity was located in a tubulo-vesicular membrane fraction. Enzyme activity was ten fold greater in this fraction than in a crude parietal cell homogenate. The substituted benzimidazoles, omeprazole and picoprazole, inhibited K+-ATPase (IC50 1.8 +/- 0.5 mumol l-1 and 3.1 +/- 0.4 mumol l-1, respectively). Detailed kinetic analysis indicated that these compounds were non-competitive and reversible inhibitors of the enzyme. In contrast cimetidine and verapamil were without effect on the enzyme. The relevance of the inhibition of K+-ATPase to the antisecretory activity of the benzimidazoles, in experimental animals and man, is discussed. PMID:6146367

Embedding the dynamics of a single delay system into a feed-forward ring.

Science.gov (United States)

Klinshov, Vladimir; Shchapin, Dmitry; Yanchuk, Serhiy; Wolfrum, Matthias; D'Huys, Otti; Nekorkin, Vladimir

2017-10-01

We investigate the relation between the dynamics of a single oscillator with delayed self-feedback and a feed-forward ring of such oscillators, where each unit is coupled to its next neighbor in the same way as in the self-feedback case. We show that periodic solutions of the delayed oscillator give rise to families of rotating waves with different wave numbers in the corresponding ring. In particular, if for the single oscillator the periodic solution is resonant to the delay, it can be embedded into a ring with instantaneous couplings. We discover several cases where the stability of a periodic solution for the single unit can be related to the stability of the corresponding rotating wave in the ring. As a specific example, we demonstrate how the complex bifurcation scenario of simultaneously emerging multijittering solutions can be transferred from a single oscillator with delayed pulse feedback to multijittering rotating waves in a sufficiently large ring of oscillators with instantaneous pulse coupling. Finally, we present an experimental realization of this dynamical phenomenon in a system of coupled electronic circuits of FitzHugh-Nagumo type.

Beam monitors and transverse feedback system of TRISTAN Main Ring

International Nuclear Information System (INIS)

Ieiri, T.; Ishii, H.; Kishiro, J.; Mizumachi, Y.; Mori, K.; Nakajima, K.; Ogata, A.; Shintake, T.; Tejima, M.

1987-01-01

The construction of 30 GeV TRISTAN Main Ring (MR) started in 1983 soon after the commissioning of 8 GeV Accumulation Ring (AR). The authors prepared 392 position monitors, 6 synchrotron radiation monitors, 9 screen monitors, 2 DCCT's, 3 scrapers, 12 bunch monitors, transverse feedback systems for two beams and DC separators. Since the required monitoring devices of AR and MR are almost the same, the experiences in AR were very useful in the design of MR monitors. However, machine parameters of two rings are very different and the authors had to review the performance of each item. From the monitor point of view the most important is the difference of revolution frequency; 794.6 kHz for AR and 99.33 kHz for MR. This means that average beam current of MR is 1/8 as small as AR current with the same bunch number and intensity. Therefore, the sensitivity of each monitor must be better in MR. The second difference is that MR should be used as a collider from the beginning. Therefore they must prepare for multi-beam and multi-bunch operation

Amine-free melanin-concentrating hormone receptor 1 antagonists: Novel 1-(1H-benzimidazol-6-yl)pyridin-2(1H)-one derivatives and design to avoid CYP3A4 time-dependent inhibition.

Science.gov (United States)

Igawa, Hideyuki; Takahashi, Masashi; Shirasaki, Mikio; Kakegawa, Keiko; Kina, Asato; Ikoma, Minoru; Aida, Jumpei; Yasuma, Tsuneo; Okuda, Shoki; Kawata, Yayoi; Noguchi, Toshihiro; Yamamoto, Syunsuke; Fujioka, Yasushi; Kundu, Mrinalkanti; Khamrai, Uttam; Nakayama, Masaharu; Nagisa, Yasutaka; Kasai, Shizuo; Maekawa, Tsuyoshi

2016-06-01

Melanin-concentrating hormone (MCH) is an attractive target for antiobesity agents, and numerous drug discovery programs are dedicated to finding small-molecule MCH receptor 1 (MCHR1) antagonists. We recently reported novel pyridine-2(1H)-ones as aliphatic amine-free MCHR1 antagonists that structurally featured an imidazo[1,2-a]pyridine-based bicyclic motif. To investigate imidazopyridine variants with lower basicity and less potential to inhibit cytochrome P450 3A4 (CYP3A4), we designed pyridine-2(1H)-ones bearing various less basic bicyclic motifs. Among these, a lead compound 6a bearing a 1H-benzimidazole motif showed comparable binding affinity to MCHR1 to the corresponding imidazopyridine derivative 1. Optimization of 6a afforded a series of potent thiophene derivatives (6q-u); however, most of these were found to cause time-dependent inhibition (TDI) of CYP3A4. As bioactivation of thiophenes to form sulfoxide or epoxide species was considered to be a major cause of CYP3A4 TDI, we introduced electron withdrawing groups on the thiophene and found that a CF3 group on the ring or a Cl adjacent to the sulfur atom helped prevent CYP3A4 TDI. Consequently, 4-[(5-chlorothiophen-2-yl)methoxy]-1-(2-cyclopropyl-1-methyl-1H-benzimidazol-6-yl)pyridin-2(1H)-one (6s) was identified as a potent MCHR1 antagonist without the risk of CYP3A4 TDI, which exhibited a promising safety profile including low CYP3A4 inhibition and exerted significant antiobesity effects in diet-induced obese F344 rats. Copyright © 2016 Elsevier Ltd. All rights reserved.

Iodine-catalyzed Csp3-H functionalization of methylhetarenes: One-pot synthesis and cytotoxic evaluation of heteroarenyl-benzimidazoles and benzothiazole.

Science.gov (United States)

Baig, Mirza Feroz; Shaik, Siddiq Pasha; Nayak, V Lakshma; Alarifi, Abdullah; Kamal, Ahmed

2017-09-01

An efficient one-pot synthetic procedure has been developed for the preparation of heteroarenyl-benzimidazoles via oxidative C sp3 -H functionalization with o-phenylenediamine using I 2 -DMSO in open air from easily available starting materials. Based on a logical plan a spectrum of multi fundamental reactions like iodination, Kornblum oxidation and amination were brought into one-pot. By using this simple method a library of heteroarenyl-benzimidazoles derivatives (3a-t and 5a-g) and heteroarenyl-benzothiazole (3u) have been synthesized in good to excellent yield and screened for their cytotoxicity against a group of four human cancer cell lines. Among them 3h, 3q and 5b showed significant cytotoxic activities with an IC 50 of 1.69, 1.62 and 2.81µM respectively against lung cancer (A549) cell line. Copyright © 2017 Elsevier Ltd. All rights reserved.

Concise copper-catalyzed synthesis of tricyclic biaryl ether-linked aza-heterocyclic ring systems.

Science.gov (United States)

Mestichelli, Paola; Scott, Matthew J; Galloway, Warren R J D; Selwyn, Jamie; Parker, Jeremy S; Spring, David R

2013-11-01

A new method for the synthesis of tricyclic biaryl ether-linked ring systems incorporating seven-, eight-, and nine-membered ring amines is presented. In the presence of catalytic quantities of copper(I), readily accessible acyclic precursors undergo an intramolecular carbon-oxygen bond-forming reaction facilitated by a "templating" chelating nitrogen atom. The methodology displays a broad substrate scope, is practical, and generates rare and biologically interesting tricyclic heteroaromatic products that are difficult to access by other means.

Quantum correlations in a bipartite multiqubit spin ring system

International Nuclear Information System (INIS)

Doronin, S I; Fel’dman, E B; Kuznetsova, E I

2015-01-01

We consider a spin ring with an arbitrary number of spins on the ring and one spin in its center in a strong external magnetic field. The spins on the ring are connected by the secular dipole–dipole interactions and interact with the central spin through the Heisenberg zz-interaction. We show that the quantum discord, describing quantum correlations between the ring and the central spin, can be obtained analytically for an arbitrary number of the spins in the high-temperature approximation. We demonstrate the evolution of quantum correlations at different numbers of the spins. The contributions of longitudinal and transversal spin interactions to the quantum discord are discussed. (paper)

A Practical Green Synthesis and Biological Evaluation of Benzimidazoles Against Two Neglected Tropical Diseases: Chagas and Leishmaniasis.

Science.gov (United States)

Bandyopadhyay, Debashis; Samano, Selina; Villalobos-Rocha, Juan Carlos; Sanchez-Torres, Luvia Enid; Nogueda-Torres, Benjamin; Rivera, Gildardo; Banik, Bimal K

2017-01-01

Antimicrobial resistance is an ever-increasing problem throughout the world and has already reached severe proportions. Two very common neglected tropical diseases are Chagas' disease and leishmaniasis. Chagas' disease is a severe health problem, mainly in Latin America, causing approximately 50000 deaths a year and millions of people are infected. About 25-30% of the patients infected with Trypanosoma cruzi develop the chronic form of the disease. On the other hand, Leishmaniasis represents complex diseases with an important clinical and epidemiological diversity. It is endemic in 88 countries 72 of which are developing countries and it has been estimated that are 12 million people infected and 350 million are in areas with infection risk. On this basis, research on organic compounds that can be used against these two diseases is an important target. A very simple, green, and efficient protocol is developed in which bismuth nitrate pentahydrate is employed as a Lewis acid catalyst in aqueous media under microwave irradiation for the synthesis of various 2-aryl substituted benzimidazoles from aldehydes and o-phenylenediamine. Other salient features of this protocol include milder conditions, atom-economy, easy extraction, and no wastes. Nine 1H-benzimidazole derivatives (1-9) with substituents at positions 2 and 5 were synthesized and the structure of the compounds was elucidated by spectroscopic methods. The compounds were screened to identify whether they posses pharmacological activity against Chagas' disease and leishmaniasis. Compound 8 showed better activity than the control Nifurtimox against INC-5 Trypanosoma cruzi strain whereas compounds 3 and 9 have demonstrated potent leshmanicidal activity. A systematic green synthetic procedure and in vitro biological evaluation of nine 1H-benzimidazoles are described. Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.org.

Antituberculosis: Synthesis and Antimycobacterial Activity of Novel Benzimidazole Derivatives

Directory of Open Access Journals (Sweden)

Yeong Keng Yoon

2013-01-01

Full Text Available A total of seven novel benzimidazoles were synthesized by a 4-step reaction starting from 4-fluoro-3-nitrobenzoic acid under relatively mild reaction conditions. The synthesized compounds were screened for their antimycobacterial activity against M. tuberculosis H37Rv (MTB-H37Rv and INH-resistant M. tuberculosis (INHR-MTB strains using agar dilution method. Three of them displayed good activity with MIC of less than 0.2 μM. Compound ethyl 1-(2-(4-(4-(ethoxycarbonyl-2-aminophenylpiperazin-1-ylethyl-2-(4-(5-(4-fluorophenylpyridin-3-ylphenyl-1H-benzo[d]imidazole-5-carboxylate (5g was found to be the most active with MIC of 0.112 μM against MTB-H37Rv and 6.12 μM against INHR-MTB, respectively.

Determination of benzimidazoles in meat samples by capillary zone electrophoresis tandem mass spectrometry following dispersive liquid-liquid microextraction.

Science.gov (United States)

Tejada-Casado, Carmen; Moreno-González, David; Lara, Francisco J; García-Campaña, Ana M; Del Olmo-Iruela, Monsalud

2017-03-24

A novel method based on capillary zone electrophoresis-tandem mass spectrometry has been proposed and validated for the identification and simultaneous quantification of twelve benzimidazoles in meat samples. Electrophoretic separation was carried out using 500mM formic acid (pH 2.2) as background electrolyte and applying a voltage of 25kV at 25°C. In order to improve the sensitivity, stacking mode injection was applied, using as injection solvent a mixture of 30:70 acetonitrile/water at 50mbar for 75s. Sensitivity enhancement factors from 74 to 317 were obtained under these conditions. Detection using an ion trap as analyzer, operating in multiple reactions monitoring mode was employed. The main MS/MS parameters as well as the composition of the sheath liquid and other electrospray variables were optimized in order to obtain the highest sensitivity and precision in conjunction with an unequivocal identification. The method was applied to poultry and pork muscle samples. The deproteinization of samples and extraction of benzimidazoles was carried out with acetonitrile. MgSO 4 and NaCl were added as salting-out agents. Subsequently, dispersive liquid-liquid microextraction was applied as clean up procedure. The organic layer (acetonitrile, used as dispersant) containing the benzimidazoles was mixed with the extractant (chloroform) and both were injected in water, producing a cloudy solution. Recoveries for fortified samples were higher than 70%, with relative standard deviations lower than 16% were obtained in all cases. The limits of detection were below 3μgkg -1 , demonstrating the applicability of this fast, simple, and environmentally friendly method. Copyright © 2017 Elsevier B.V. All rights reserved.

Photometric Analysis of the Jovian Ring System and Modeling of Ring Origin and Evolution

Science.gov (United States)

Esposito, L. W.

2003-01-01

We have successfully completed the work described in our proposal. The work supported by this grant resulted in the publication of the following paper: Brooks, S. M., L. W. Esposito, M. R. Showalter, and H. B. Throop. 2002. The size distribution of Jupiter's main ring from Galileo imaging and spectroscopy. Icarus, in press. This was also the major part of Dr. Shawn Brooks PhD dissertation. Dr. Brooks gave oral presentations on this work at the Lunar and Planetary Conference, the annual meetings of the Division for Planetary Sciences of the American Astronomical Society, the annual meetings of the European Geophysical Society, the international Jupiter Conference in Boulder, the Jupiter after Galileo and Cassini Conference in Lisbon and to the Working Group in Non-Linear Dynamics in Potsdam, Germany. This work was reviewed in: Esposito, L. W. 2002. Planetary rings. Rep. hog. Phys. 65, 1741-1783. Planetary rings. LASP reprint 874. Online at http://stacks.iop.org/RoPP/65/1741. Dr. Esposito gave presentations at schools and over the internet on the results of this work. Dr. Brooks lectured in undergraduate and graduate classes on Jupiter's rings, and on the meaning of his research. In August 2003, Dr. Shawn Brooks received the Phd degree from the University of Colorado in Astrophysical and Planetary Sciences.

Linear and nonlinear optical susceptibilities in a laterally coupled quantum-dot–quantum-ring system

International Nuclear Information System (INIS)

Zeng, Zaiping; Garoufalis, Christos S.; Baskoutas, Sotirios

2014-01-01

Linear and nonlinear optical susceptibilities in a laterally coupled quantum-dot–quantum-ring system have been theoretically studied. In general, we find that the structure parameters of the coupled system significantly affect the optical susceptibilities. The enhancement of the coupling effects between the dot and ring is found to increase considerably the optical susceptibilities and redshift drastically the transition energies. Comparing to the linear susceptibility, the nonlinear optical susceptibility is found to be more sensitive to the variation of the structure parameters. A comprehensive analysis of the electron probability density movement with respect to the modification of the structure parameters is provided, which offers a unique perspective of the ground-state localization. - Highlights: • Optical susceptibilities in a quantum-dot–quantum-ring system are studied. • The structure parameters significantly affect the optical susceptibilities. • The enhancement of the coupling effects increases the optical susceptibilities. • The nonlinear susceptibility is more sensitive to the change in structure parameters. • A comprehensive analysis of the electron probability density movement is provided

Explicitly-correlated ring-coupled-cluster-doubles theory: Including exchange for computations on closed-shell systems

Energy Technology Data Exchange (ETDEWEB)

Hehn, Anna-Sophia; Holzer, Christof; Klopper, Wim, E-mail: klopper@kit.edu

2016-11-10

Highlights: • Ring-coupled-cluster-doubles approach now implemented with exchange terms. • Ring-coupled-cluster-doubles approach now implemented with F12 functions. • Szabo–Ostlund scheme (SO2) implemented for use in SAPT. • Fast convergence to the limit of a complete basis. • Implementation in the TURBOMOLE program system. - Abstract: Random-phase-approximation (RPA) methods have proven to be powerful tools in electronic-structure theory, being non-empirical, computationally efficient and broadly applicable to a variety of molecular systems including small-gap systems, transition-metal compounds and dispersion-dominated complexes. Applications are however hindered due to the slow basis-set convergence of the electron-correlation energy with the one-electron basis. As a remedy, we present approximate explicitly-correlated RPA approaches based on the ring-coupled-cluster-doubles formulation including exchange contributions. Test calculations demonstrate that the basis-set convergence of correlation energies is drastically accelerated through the explicitly-correlated approach, reaching 99% of the basis-set limit with triple-zeta basis sets. When implemented in close analogy to early work by Szabo and Ostlund [36], the new explicitly-correlated ring-coupled-cluster-doubles approach including exchange has the perspective to become a valuable tool in the framework of symmetry-adapted perturbation theory (SAPT) for the computation of dispersion energies of molecular complexes of weakly interacting closed-shell systems.

The fluid systems for the SLD Cherenkov ring imaging detector

International Nuclear Information System (INIS)

Abe, K.; Hasegawa, K.; Hasegawa, Y.; Iwasaki, Y.; Suekane, F.; Yuta, H.; Baird, K.; Jacques, P.; Kalelkar, M.; Plano, R.; Stamer, P.; Word, G.; Bean, A.; Caldwell, D.O.; Duboscq, J.; Huber, J.; Lu, A.; Mathys, L.; McHugh, S.; Yellin, S.; Ben-David, R.; Manly, S.; Snyder, J.; Turk, J.; Cavalli-Sforza, M.; Coyle, P.; Coyne, D.; Gagnon, P.; Liu, X.; Schneider, M.; Williams, D.A.; Coller, J.; Shank, J.T.; Whitaker, J.S.; d'Oliveira, A.; Johnson, R.A.; Martinez, J.; Nussbaum, M.; Santha, A.K.S.; Sokoloff, M.D.; Stockdale, I.; Wilson, R.J.

1992-10-01

We describe the design and operation of the fluid delivery, monitor and control systems for the SLD barrel Cherenkov Ring Imaging Detector (CRID). The systems deliver drift gas (C 2 H 6 + TMAE), radiator gas (C 5 F 12 + N 2 ) and radiator liquid (C 6 F 14 ). Measured critical quantities such as electron lifetime in the drift gas and ultra-violet (UV) transparencies of the radiator fluids, together with the operational experience, are also reported

Rf systems for high-energy e/sup /minus//e/sup /plus// storage rings

International Nuclear Information System (INIS)

Allen, M.A.; Wilson, P.B.

1974-01-01

Electron or positron beams in a storage ring radiate electromagnetic energy at a rate proportional to the fourth power of the recirculating energy, and this loss must be supplied by an rf system. Furthermore, a substantial overvoltage is required to contain the stored beam against losses due to quantum fluctuations in the emitted photons. As an example, an improvement program, SPEAR II, is now underway to increase the energy of the SPEAR ring to 4.5 GeV. At this energy, the radiation loss per turn is 2.8 MeV, and to maintain a reasonable lifetime against quantum fluctuations, a peak voltage of 7.5 MeV is required. Thus, the SPEAR II rf system is similar to a continuously-operating 7.5 MeV linear accelerator. Furthermore, the available straight-section space in the ring which is suitable for containing the accelerating structures is limited, and this means that a cavity design must be sought with a high shunt impedance per losses will be held to a reasonable level. In the case of SPEAR, about 9 meters of straight section space is available for accelerating cavities, requiring a gradient of close to 1 MV per meter. The PEP 15-GeV ring would require peak accelerating voltages of around 50 MV, with about 60 meters of straight-section space available for accelerating structures. 8 refs

Active interlock system for high power insertion devices in the x-ray ring

International Nuclear Information System (INIS)

Anon.

1991-01-01

In modern synchrotron radiation rings photon beams generated by high power insertion devices (IDs) may be sufficiently intense to cause severe thermal damage to the machine vacuum chamber if mis-steered. Thus when operating a storage ring with the IDs, great care must be exercised to prevent mis-steering of the electron beam orbit. At present, the X-ray ring operates with three IDs, namely two hybrid wigglers (HBW) at X-21 and X-25,a nd a 5-Tesla superconducting wiggler at X-17. All wigglers are located in low-beta straight sections. In the straight sections. In the straight sections, beam orbit may be deflected by as much as ±8 mrad without scraping the chamber wall. For various reasons it was not possible to design the X-ray ring vacuum chamber to be safe under all possible operating conditions, however, the chamber is safe for i < 7 mA, all horizontal beam deflection angles and for vertical angles < ± 2.5 mrad. To protect the machine vacuum chamber from damage due to mis-steered beams, and interlock system has been developed and installed. This system utilizes active beam position detectors which continuously monitor beam motion in each of the ID straight sections and logic circuitry which interrupts the RF and dumps the stored beam in the case of a fault

Crystal structures of HIV-1 nonnucleoside reverse transcriptase inhibitors: N-benzyl-4-methyl-benzimidazoles

Science.gov (United States)

Ziółkowska, Natasza E.; Michejda, Christopher J.; Bujacz, Grzegorz D.

2009-07-01

HIV-1 nonnucleoside reverse transcriptase inhibitors are potentially specific and effective drugs in AIDS therapy. The presence of two aromatic systems with an angled orientation in the molecule of the inhibitor is crucial for interactions with HIV-1 RT. The inhibitor drives like a wedge into the cluster of aromatic residues of RT HIV-1 and restrains the enzyme in a conformation that blocks the chemical step of nucleotide incorporation. Structural studies provide useful information for designing new, more active inhibitors. The crystal structures of four NNRTIs are presented here. The investigated compounds are derivatives of N-benzyl-4-methyl-benzimidazole with various aliphatic and aromatic substituents at carbon 2 positions and a 2,6-dihalogeno-substituted N-benzyl moiety. Structural data reported here show that the conformation of the investigated compounds is relatively rigid. Such feature is important for the nonnucleoside inhibitor binding to HIV-1 reverse transcriptase.

The LSU Electron Storage Ring, the first commercially-built storage ring

International Nuclear Information System (INIS)

Sah, R.

1990-01-01

The Brobeck Division of Maxwell Laboratories, Inc., is building the first industrially-produced storage ring. It will be located at Louisiana State University (LSU) at the Center for Advanced Microstructures and Devices (CAMD) in Baton Rouge. The purpose of this electron storage ring is to provide intense beams of x-rays to advance the state-of-the-art in lithography and to permit research in a broad area. This facility consists of a 1.2 GeV, 400 mA electron storage ring with a 200 MeV linac injector. The magnet lattice is a Chasman-Green design (double-bend achromat), and the ring circumference is 55.2 meters. There are four 3.0 meter, dispersion-free straight sections, one for injection, one for the 500 MHz RF cavity, and two for possible future insertion devices. The storge ring construction project is in the detailed-design stage, and many systems are in the initial stages of fabrication. 4 figs., 1 tab

The thermodynamic of complex formation in system of the Fe(III)-Fe(II)-benzimidazole-water in the inflation of ion strength in the formation of co-ordination compounds in the 288 K

International Nuclear Information System (INIS)

Nazarova, Kh.D.; Rajabov, U.R.; Yusupov, Z.N.

2005-01-01

With the Method of Oxredmatrion with application of the Oxidation Function in the Temperature 288 K and ion strength 0.1; 0.25; 0.50 and 1.00 in the Water solution of Benzimidazole been obtained the Formation Constants of the Coordination and their dependence with ion strength

Saturn's Ring: Pre-Cassini Status and Mission Goals

Science.gov (United States)

Cuzzi, Jeff N.; DeVincenzi, Donald L. (Technical Monitor)

1999-01-01

In November 1980, and again in August 1981, identical Voyager spacecraft flew through the Saturn system, changing forever the way we think about planetary rings. Although Saturn's rings had been the only known ring system for three centuries, a ring system around Uranus had been discovered by stellar occultations from Earth in 1977, and the nearly transparent ring of Jupiter was imaged by Voyager in 1979 (the presence of material there had been inferred from charged particle experiments on Pioneer 10 and 11 several years earlier). While Saturn had thus temporarily lost its uniqueness as having the only ring system, with Voyager it handily recaptured the role of having the most fascinating one. The Voyager breakthroughs included spiral density and bending waves such as cause galactic structure; ubiquitous fine-scale radial 'irregular' structure, with the appearance of record-grooves; regional and local variations in particle color; complex, azimuthally variable ring structure; empty gaps in the rings, some containing very regular, sharp-edged, elliptical rings and one containing both a small moonlet and incomplete arcs of dusty material; and shadowy 'spokes' that flicker across the main rings. One of the paradigm shifts of this period was the realization that many aspects of planetary rings, and even the ring systems themselves, could be 'recent' on geological timescales. These early results are reviewed and summarized in the Arizona Space Science series volumes 'Saturn'. (An excellent review of ring dynamics at a formative stage is by Goldreich and Tremaine.) From the mid 1980's to the time of this writing, progress has been steady, while at a less heady pace, and some of the novel ring properties revealed by Voyager 1 and 2 are beginning to be better understood. It is clearly impossible to cite, much less review, every advance over the last decade; however, below we summarize the main advances in understanding of Saturn's rings since the mid 1980's, in the context

Synthesis of pyrido[1,2-a]benzimidazoles and other fused imidazole derivatives with a bridgehead nitrogen atom

Science.gov (United States)

Begunov, Roman S.; Ryzvanovich, Galina A.

2013-01-01

Main methods for the synthesis of fused imidazole derivatives with a bridgehead nitrogen atom are systematically considered and summarized. The reaction mechanisms that underlie the methods for the synthesis of pyrido[1,2-a]benzimidazoles and related compounds are described. Biological properties and mechanisms of the biological activity of fused azaheterocycles are discussed. The bibliography includes 152 references.

Construction of vacuum system for Tristan accumulation ring

International Nuclear Information System (INIS)

Ishimaru, H.; Horikoshi, G.; Kobayashi, M.; Kubo, T.; Mizuno, H.; Momose, T.; Narushima, K.; Watanabe, H.; Yamaguchi, H.

1983-01-01

An all aluminum-alloy vacuum system for the TRISTAN accumulation ring is now under construction. Aluminum and aluminum alloys are preferred materials for ultrahigh vacuum systems of large electron storage rings because of their good thermal conductivity, extremely low outgassing rate, and low residual radioactivity. Vacuum beam chambers for the dipole and quadrupole magnets are extruded using porthole dies. The aluminum alloy 6063-T6 provides superior performance in extrusion. For ultrahigh vacuum performance, a special extrusion technique is applied which, along with the outgassing procedure used, is described in detail. Aluminum alloy 3004 seamless elliptical bellows are inserted between the dipole and quadrupole magnet chambers. These bellows are produced by the hydraulic forming of a seamless tube. The seamless bellows and the beam chambers are joined by fully automatic welding. The ceramic chambers for the kicker magnets, the fast bump magnets, and the slow beam intensity monitor are inserted in the aluminum alloy beam chambers. The ceramic chamber (98% alumina) and elliptical bellows are brazed with brazing sheets (4003-3003-4003) in a vacuum furnace. The brazing technique is described. The inner surface of the ceramic chamber is coated with a TiMo alloy by vacuum evaporation to permit a smooth flow of the RF wall current. Other suitable aluminum alloy components, including fittings, feedthroughs, gauges, optical windows, sputter ion pumps, turbomolecular pumps, and valves have been developed; their fabrication is described

Estimation of the cost of large-scale school deworming programmes with benzimidazoles

Science.gov (United States)

Montresor, A.; Gabrielli, A.F.; Engels, D.

2017-01-01

Summary This study estimates the cost of distributing benzimidazole tablets in the context of school deworming programmes: we analysed studies reporting the cost of school deworming from seven countries in four WHO regions. The estimated cost for drug procurement to cover one million children (including customs clearance and international transport) is approximately US$20 000. The estimated financial costs (including the cost of training of personnel, drug transport, social mobilization and monitoring) is, on average, equivalent to US$33 000 per million school-age children with minimal variation in different countries and continents. The estimated economic costs of distribution (including the time spent by teachers, and health personnel at central, provincial and district level) to cover one million children approximately corresponds to US$19 000. This study shows the minimal cost of school deworming activities, but also shows the significant contribution (corresponding to a quarter of the entire cost of the programme) provided by health and education systems in endemic countries even in the case of drug donations and donor support of distribution costs. PMID:19926104

The New Horizons and Hubble Space Telescope search for rings, dust, and debris in the Pluto-Charon system

Science.gov (United States)

Lauer, Tod R.; Throop, Henry B.; Showalter, Mark R.; Weaver, Harold A.; Stern, S. Alan; Spencer, John R.; Buie, Marc W.; Hamilton, Douglas P.; Porter, Simon B.; Verbiscer, Anne J.; Young, Leslie A.; Olkin, Cathy B.; Ennico, Kimberly; New Horizons Science Team

2018-02-01

We conducted an extensive search for dust or debris rings in the Pluto-Charon system before, during, and after the New Horizons encounter in July 2015. Methodologies included attempting to detect features by back-scattered light during the approach to Pluto (phase angle α ∼ 15°), in situ detection of impacting particles, a search for stellar occultations near the time of closest approach, and by forward-scattered light imaging during departure (α ∼ 165°). An extensive search using the Hubble Space Telescope (HST) prior to the encounter also contributed to the final ring limits. No rings, debris, or dust features were observed, but our new detection limits provide a substantially improved picture of the environment throughout the Pluto-Charon system. Searches for rings in back-scattered light covered the range 35,000-250,000 km from the system barycenter, a zone that starts interior to the orbit of Styx, the innermost minor satellite, and extends out to four times the orbital radius of Hydra, the outermost known satellite. We obtained our firmest limits using data from the New Horizons LORRI camera in the inner half of this region. Our limits on the normal I/F of an unseen ring depends on the radial scale of the rings: 2 ×10-8 (3σ) for 1500 km wide rings, 1 ×10-8 for 6000 km rings, and 7 ×10-9 for 12,000 km rings. Beyond ∼ 100, 000 km from Pluto, HST observations limit normal I/F to ∼ 8 ×10-8 . Searches for dust features from forward-scattered light extended from the surface of Pluto to the Pluto-Charon Hill sphere (rHill = 6.4 ×106 km). No evidence for rings or dust clouds was detected to normal I/F limits of ∼ 8.9 ×10-7 on ∼ 104 km scales. Four stellar occulation observations also probed the space interior to Hydra, but again no dust or debris was detected. The Student Dust Counter detected one particle impact 3.6 × 106 km from Pluto, but this is consistent with the interplanetary space environment established during the cruise of New

Comparison of Conventional and Microwave-assisted Synthesis of Benzimidazole Derivative from Citronellal in Kaffir lime oil (Citrus hystrix DC.)

Science.gov (United States)

Warsito, W.; Noorhamdani, A. S.; Suratmo; Dwi Sapri, R.; Alkaroma, D.; Azhar, A. Z.

2018-04-01

Simple method has been used for the synthesis of benzimidazole derivative from citronellal in kaffir lime oil under microwave irradiation. These compounds were synthesized also by conventional heating for comparison. In addtion, microwave-assited synthesis was also compared between using to dichloromethane and methanol solvents with variation of reaction time for 30 to 70 minutes and 4 to 12 h for conventional heating. The 2-citronellyl benzimidazole compound synthesized were characterised by FT-IR, GC-MS, 1H and 13C NMR spectroscopy. Comparison between conventional and microwave-assisted synthesis was done by comparing between correlation of reaction time and percentage yield. The time optimum of microwave-assisted and conventional synthesis using dichloromethane solvent respectively at 60 minutes (yield 19.23%) and 8 hours (yield 11.54%). In addition, microwave-assited synthesis increasing 157.81 times compared by conventional heating. While using methanol solvent tends to increase linearly however the percentage of yield only 0.77 times of synthesis using dichloromethane solvent.

1-Benzyl-2-Phenylbenzimidazole (BPB, a Benzimidazole Derivative, Induces Cell Apoptosis in Human Chondrosarcoma through Intrinsic and Extrinsic Pathways

Directory of Open Access Journals (Sweden)

Ju-Fang Liu

2012-12-01

Full Text Available In this study, we investigated the anticancer effects of a new benzimidazole derivative, 1-benzyl-2-phenyl -benzimidazole (BPB, in human chondrosarcoma cells. BPB-mediated apoptosis was assessed by the MTT assay and flow cytometry analysis. The in vivo efficacy was examined in a JJ012 xenograft model. Here we found that BPB induced apoptosis in human chondrosarcoma cell lines (JJ012 and SW1353 but not in primary chondrocytes. BPB induced upregulation of Bax, Bad and Bak, downregulation of Bcl-2, Bid and Bcl-XL and dysfunction of mitochondria in chondrosarcoma. In addition, BPB also promoted cytosolic releases AIF and Endo G. Furthermore, it triggered extrinsic death receptor-dependent pathway, which was characterized by activating Fas, FADD and caspase-8. Most importantly, animal studies revealed a dramatic 40% reduction in tumor volume after 21 days of treatment. Thus, BPB may be a novel anticancer agent for the treatment of chondrosarcoma.

A bioinspired catalytic aerobic oxidative C-H functionalization of primary aliphatic amines: synthesis of 1,2-disubstituted benzimidazoles.

Science.gov (United States)

Nguyen, Khac Minh Huy; Largeron, Martine

2015-09-01

Aerobic oxidative CH functionalization of primary aliphatic amines has been accomplished with a biomimetic cooperative catalytic system to furnish 1,2-disubstituted benzimidazoles that play an important role as drug discovery targets. This one-pot atom-economical multistep process, which proceeds under mild conditions, with ambient air and equimolar amounts of each coupling partner, constitutes a convenient environmentally friendly strategy to functionalize non-activated aliphatic amines that remain challenging substrates for non-enzymatic catalytic aerobic systems. © 2015 The Authors. Published by Wiley-VCH Verlag GmbH & Co. KGaA. This is an open access article under the terms of Creative Commons Attribution NonCommercial-NoDerivs License, which permits use and distribution in any medium, provided the original work is properly cited, the use is non-commercial and no modifications or adaptations are made.

Synthesis of 4-(3-t-butylamino-2-hydroxypropoxy)- benzimidazol -2 (/sup 11/C)-one (CGP 12177)

Energy Technology Data Exchange (ETDEWEB)

Boullais, C; Crouzel, C; Syrota, A

1986-05-01

4-(3-t-butylamino-2-hydroxypropoxy)-benzimidazol-2 (/sup 11/C)-one (CGP 12177) was synthesized in a short time (30 min) and with a specific activity of 130 mCi/..mu..Mo1 for ..beta.. receptor studies by the positron emission tomography. The radioactive reagent was /sup 11/C-phosgene and the starting material 1-(3-t-butylamino-2-hydroxypropoxy)-2,3-diamino benzene.

Ring faults and ring dikes around the Orientale basin on the Moon.

Science.gov (United States)

Andrews-Hanna, Jeffrey C; Head, James W; Johnson, Brandon; Keane, James T; Kiefer, Walter S; McGovern, Patrick J; Neumann, Gregory A; Wieczorek, Mark A; Zuber, Maria T

2018-08-01

The Orientale basin is the youngest and best-preserved multiring impact basin on the Moon, having experienced only modest modification by subsequent impacts and volcanism. Orientale is often treated as the type example of a multiring basin, with three prominent rings outside of the inner depression: the Inner Rook Montes, the Outer Rook Montes, and the Cordillera. Here we use gravity data from NASA's Gravity Recovery and Interior Laboratory (GRAIL) mission to reveal the subsurface structure of Orientale and its ring system. Gradients of the gravity data reveal a continuous ring dike intruded into the Outer Rook along the plane of the fault associated with the ring scarp. The volume of this ring dike is ~18 times greater than the volume of all extrusive mare deposits associated with the basin. The gravity gradient signature of the Cordillera ring indicates an offset along the fault across a shallow density interface, interpreted to be the base of the low-density ejecta blanket. Both gravity gradients and crustal thickness models indicate that the edge of the central cavity is shifted inward relative to the equivalent Inner Rook ring at the surface. Models of the deep basin structure show inflections along the crust-mantle interface at both the Outer Rook and Cordillera rings, indicating that the basin ring faults extend from the surface to at least the base of the crust. Fault dips range from 13-22° for the Cordillera fault in the northeastern quadrant, to 90° for the Outer Rook in the northwestern quadrant. The fault dips for both outer rings are lowest in the northeast, possibly due to the effects of either the direction of projectile motion or regional gradients in pre-impact crustal thickness. Similar ring dikes and ring faults are observed around the majority of lunar basins.

Hydrogen-bond-driven electrophilic activation for selectivity control: scope and limitations of fluorous alcohol-promoted selective formation of 1,2-disubstituted benzimidazoles and mechanistic insight for rationale of selectivity.

Science.gov (United States)

Chebolu, Rajesh; Kommi, Damodara N; Kumar, Dinesh; Bollineni, Narendra; Chakraborti, Asit K

2012-11-16

Hydrogen-bond-driven electrophilic activation for selectivity control during competitive formation of 1,2-disubstituted and 2-substituted benzimidazoles from o-phenylenediamine and aldehydes is reported. The fluorous alcohols trifluoroethanol and hexafluoro-2-propanol efficiently promote the cyclocondensation of o-phenylenediamine with aldehydes to afford selectively the 1,2-disubstituted benzimidazoles at rt in short times. A mechanistic insight is invoked by NMR, mass spectrometry, and chemical studies to rationalize the selectivity. The ability of the fluorous alcohols in promoting the reaction and controlling the selectivity can be envisaged from their better hydrogen bond donor (HBD) abilities compared to that of the other organic solvents as well as of water. Due to the better HBD values, the fluorous alcohols efficiently promote the initial bisimine formation by electrophilic activation of the aldehyde carbonyl. Subsequently the hydrogen-bond-mediated activation of the in situ-formed bisimine triggers the rearrangement via 1,3-hydride shift to form the 1,2-disubstituted benzimidazoles.

Investigation of REE perchlorates complexing with benzimidazole in aqua-dioxane media. Issledovanie kompleksoobrazovaniya perkhloratov RZEh s benzimidazolom v vodno-dioksanovoj srede

Energy Technology Data Exchange (ETDEWEB)

Akhrimenko, Z M; Panyushkin, V T; Ishbulatova, S K [Kubanskij Gosudarstvennyj Univ., Krasnodar (Russian Federation)

1992-01-01

Stability constant (K[sub 1]) of complexes of rare earth perchlorates with benzimidazole were determined by the method of pH-metric titration. Nonmonotonous change in lgK[sub 1] with rare earth ordinal number increase was revealed.

The 2D Selfassembly of Benzimidazole and its Co-crystallization

Science.gov (United States)

Costa, Paulo; Teeter, Jacob; Kunkel, Donna; Sinitskii, Alexander; Enders, Axel

Benzimidazoles (BI) are organic molecules that form ferroelectric crystals. Key to their ferroelectric behavior are the switchable N . . . HN type bonds and how they couple to the electron system of the molecules. We attempted to crystallize BI on various metal surfaces and studied them using STM. We observed that on Au and Ag, BI joins into zipper chains characteristic of its bulk structure that can pack into a continuous 2D layer. Because the dipole of BI lies in the direction of its switchable hydrogen bond, these zippers should in principle have reversible polarizations that point along the direction they run. BI's crystallization is reminiscent to how croconic acid (CA) crystallizes in 2D using O . . . HO bonding, suggesting that these molecules may be able to co-crystallize through OH . . . N bonds. This would present the opportunity to modify BI's properties, such as the energy needed to switch a hydrogen from a donor to acceptor site. When co-deposited, CA and BI successfully combine into a co-crystal formed by building blocks consisting of 2 CA and 2 BI molecules. These findings demonstrate the usefulness of using STM as a preliminary check to verify if two molecules are compatible with each other without having to attempt crystallization with multiple solvents and mixing methods.

Design, synthesis, molecular docking and biological evaluation of new dithiocarbamates substituted benzimidazole and chalcones as possible chemotherapeutic agents.

Science.gov (United States)

Bacharaju, Keerthana; Jambula, Swathi Reddy; Sivan, Sreekanth; Jyostnatangeda, Saritha; Manga, Vijjulatha

2012-05-01

A series of novel dithiocarbamates with benzimidazole and chalcone scaffold have been designed synthesised and evaluated for their antimitotic activity. Compounds 4c and 9d display the most promising antimitotic activity with IC(50) of 1.66 μM and 1.52 μM respectively. Copyright © 2012 Elsevier Ltd. All rights reserved.

Synthesis and Anti-inflammatory Evaluation of Novel Benzimidazole and Imidazopyridine Derivatives.

Science.gov (United States)

Chen, Gaozhi; Liu, Zhiguo; Zhang, Yali; Shan, Xiaoou; Jiang, Lili; Zhao, Yunjie; He, Wenfei; Feng, Zhiguo; Yang, Shulin; Liang, Guang

2013-01-10

Sepsis, an acute inflammatory disease, remains the most common cause of death in intensive care units. A series of benzimidazole and imidazopyridine derivatives were synthesized and screened for anti-inflammatory activities, and the imidazopyridine series showed excellent inhibition of the expression of inflammatory cytokines in LPS-stimulated macrophages. Compounds X10, X12, X13, X14, and X15 inhibited TNF-α and IL-6 release in a dose-dependent manner, and X12 showed no cytotoxicity in hepatic cells. Furthermore, X12 exhibited a significant protection against LPS-induced septic death in mouse models. Together, these data present a series of new imidazopyridines with potential therapeutic effects in acute inflammatory diseases.

Methodology for determination of benzimidazolic fungicides residues in strawberry and lettuce by HPLC-DAD

International Nuclear Information System (INIS)

Dangond Araujo, Jose Jairo; Guerrero dallos, Jairo Arturo

2006-01-01

systemic fungicides like benzimidazolic compounds are used to protect several crops of fruits and vegetables. in this work a new method for analysis of Benomyl, carbendazim and thiabendazol in strawberry and lettuce by high performance liquid chromatography with diode array detector (HPLC-DAD) was validated. benomyl residues were determined after its conversion to carbendazim. pesticide residues were extracted from strawberry and lettuce samples with ethyl acetate and these extracts were cleaned up by gel permeation chromatography (GPC). final determination was carried out by HPLC-DAD in reverse phase column. the method is selective, specific, precise and accurate. the calibration curves show linearity over concentration range of 1.24 to 6.19 mg/kg, with detection limits of 0.40 and 0.27 mg/kg and quantification limits of 1.35 and 0.81 mg/kg for carbendazim and thiabendazole respectively. the recovery experiments yielding averages of 90 %. n o residues of these compounds were found in collected samples from specific areas of Cundinamarca, Colombia

NaHSO4-SiO2-Promoted Solvent-Free Synthesis of Benzoxazoles, Benzimidazoles, and Benzothiazole Derivatives

Directory of Open Access Journals (Sweden)

K. Ravi Kumar

2013-01-01

Full Text Available An efficient protocol has been developed for the preparation of a library of benzoxazole, benzimidazole, and benzothiazole derivatives from reactions of acyl chlorides with o-substituted aminoaromatics in the presence of catalytic amount of silica-supported sodium hydrogen sulphate under solvent-free conditions. Simple workup procedure, high yield, easy availability, reusability, and use of ecofriendly catalyst are some of the striking features of the present protocol.

Conceptual Design of ILC Damping Ring Wiggler Straight Vacuum System

International Nuclear Information System (INIS)

Marks, S.; Kennedy, K.; Plate, D.; Schlueter, R.D.; Zisman, M.

2007-01-01

The positron and electron damping rings for the International Linear Collider will contain long straight sections consisting of twenty wiggler/quadrupole pairs. The wigglers will be based upon the CESR superconducting design. There are a number of challenges associated with the design of the wiggler straight vacuum system, in particular, the absorption of photon power generated by the wigglers. This paper will present the overall conceptual design of the wiggler straight vacuum system developed for the ILC Reference Design Report. Particular emphasis will be placed on photon power load calculations and the absorber design

Saturn's Rings Edge-on

Science.gov (United States)

1995-01-01

In one of nature's most dramatic examples of 'now-you see-them, now-you-don't', NASA's Hubble Space Telescope captured Saturn on May 22, 1995 as the planet's magnificent ring system turned edge-on. This ring-plane crossing occurs approximately every 15 years when the Earth passes through Saturn's ring plane.For comparison, the top picture was taken by Hubble on December 1, 1994 and shows the rings in a more familiar configuration for Earth observers.The bottom picture was taken shortly before the ring plane crossing. The rings do not disappear completely because the edge of the rings reflects sunlight. The dark band across the middle of Saturn is the shadow of the rings cast on the planet (the Sun is almost 3 degrees above the ring plane.) The bright stripe directly above the ring shadow is caused by sunlight reflected off the rings onto Saturn's atmosphere. Two of Saturn's icy moons are visible as tiny starlike objects in or near the ring plane. They are, from left to right, Tethys (slightly above the ring plane) and Dione.This observation will be used to determine the time of ring-plane crossing and the thickness of the main rings and to search for as yet undiscovered satellites. Knowledge of the exact time of ring-plane crossing will lead to an improved determination of the rate at which Saturn 'wobbles' about its axis (polar precession).Both pictures were taken with Hubble's Wide Field Planetary Camera 2. The top image was taken in visible light. Saturn's disk appears different in the bottom image because a narrowband filter (which only lets through light that is not absorbed by methane gas in Saturn's atmosphere) was used to reduce the bright glare of the planet. Though Saturn is approximately 900 million miles away, Hubble can see details as small as 450 miles across.The Wide Field/Planetary Camera 2 was developed by the Jet Propulsion Laboratory and managed by the Goddard Spaced Flight Center for NASA's Office of Space Science.This image and other images and

TRANSIT MODEL OF PLANETS WITH MOON AND RING SYSTEMS

International Nuclear Information System (INIS)

Tusnski, Luis Ricardo M.; Valio, Adriana

2011-01-01

Since the discovery of the first exoplanets, those most adequate for life to begin and evolve have been sought. Due to observational bias, however, most of the discovered planets so far are gas giants, precluding their habitability. However, if these hot Jupiters are located in the habitable zones of their host stars, and if rocky moons orbit them, then these moons may be habitable. In this work, we present a model for planetary transit simulation considering the presence of moons and planetary rings around a planet. The moon's orbit is considered to be circular and coplanar with the planetary orbit. The other physical and orbital parameters of the star, planet, moon, and rings can be adjusted in each simulation. It is possible to simulate as many successive transits as desired. Since the presence of spots on the surface of the star may produce a signal similar to that of the presence of a moon, our model also allows for the inclusion of starspots. The result of the simulation is a light curve with a planetary transit. White noise may also be added to the light curves to produce curves similar to those obtained by the CoRoT and Kepler space telescopes. The goal is to determine the criteria for detectability of moons and/or ring systems using photometry. The results show that it is possible to detect moons with radii as little as 1.3 R ⊕ with CoRoT and 0.3 R ⊕ with Kepler.

Acetic acid-promoted condensation of o-phenylenediamine with aldehydes into 2-aryl-1-(arylmethyl-1H-benzimidazoles under microwave irradiation

Directory of Open Access Journals (Sweden)

DAVOOD AZARIF

2010-09-01

Full Text Available An efficient and simple procedure was developed for the green synthesis of various 2-aryl-1-(arylmethyl-1H-benzimidazoles in high yields by acetic acid-promoted condensation of o-phenylenediamine with aldehydes in air under microwave irradiation and transition metal catalyst-free conditions.

Ring Theory

CERN Document Server

Jara, Pascual; Torrecillas, Blas

1988-01-01

The papers in this proceedings volume are selected research papers in different areas of ring theory, including graded rings, differential operator rings, K-theory of noetherian rings, torsion theory, regular rings, cohomology of algebras, local cohomology of noncommutative rings. The book will be important for mathematicians active in research in ring theory.

SOR-ring failure

International Nuclear Information System (INIS)

Kitamura, Hideo

1981-01-01

It was in the autumn of 1976 that the SOR-ring (synchrotron radiation storage ring) has commenced the regular operation. Since then, the period when the operation was interrupted due to the failures of SOR-ring itself is in total about 8 weeks. Failures and accidents have occurred most in the vacuum system. Those failure experiences are described on the vacuum, electromagnet, radio-frequency acceleration and beam transport systems with their interrupted periods. The eleven failures in the vacuum system have been reported, such as bellows breakage in a heating-evacuating period, leakage from the bellows of straight-through valves (made in U.S.A. and Japan), and leakage from the joint flange of the vacuum system. The longest interruption was 5 weeks due to the failure of a domestically manufactured straight-through valve. The failures of the electromagnet system involve the breakage in a cooling water system, short circuit of a winding in the Q magnet power transformer, blow of a fuse protecting the deflection magnet power source by the current less than the rating, and others. The failures of the RF acceleration system include the breakage of an output electronic tube the breakage of a cavity ceramic, RF voltage fluctuation due to the contact deterioration at a cavity electrode, and the failure of grid bias power source. It is necessary to select the highly reliable components for the vacuum system because the vacuum system failures require longer time for recovery, and very likely to induce secondary and tertiary failures. (Wakatsuki, Y.)

Benzimidazole derivatives: search for GI-friendly anti-inflammatory analgesic agents

Directory of Open Access Journals (Sweden)

Monika Gaba

2015-07-01

Full Text Available Non-steroidal anti-inflammatory drugs (NSAIDs have been successfully used for the alleviation of pain and inflammation in the past and continue to be used daily by millions of patients worldwide. However, gastrointestinal (GI toxicity associated with NSAIDs is an important medical and socioeconomic problem. Local generation of various reactive oxygen species plays a significant role in the formation of gastric ulceration associated with NSAIDs therapy. Co-medication of antioxidants along with NSAIDs has been found to be beneficial in the prevention of GI injury. This paper describes the synthesis and biological evaluation of N-1-(phenylsulfonyl-2-methylamino-substituted-1H-benzimidazole derivatives as anti-inflammatory analgesic agents with lower GI toxicity. Studies in vitro and in vivo demonstrated that the antioxidant activity of the test compounds decreased GI toxicity.

Synthesis of some novel phosphorylated and thiophosphorylated benzimidazoles and benzothiazoles and their evaluation for larvicidal potential to Aedes albopictus and Culex quinquefasciatus.

Science.gov (United States)

Bandyopadhyay, Prabal; Sathe, Manisha; Tikar, Sachin N; Yadav, Ruchi; Sharma, Pratibha; Kumar, Ashok; Kaushik, M P

2014-07-01

Series of benzimidazole and benzothiazole linked phosphoramidates and phosphoramidothioates (5a-j) and benzimidazole linked phenylphosphoramidates and phenylphosphoramidothioates (10a-e) were synthesized. The title compounds were preliminary screened for mosquito larvicidal properties against Aedes albopictus and Culex quinquefasciatus at different concentration from 40 to 5 mg/L. Among the screened compounds three compounds revealed potential larvicidal effects with 100% mortality in the order of 10e>5j>5e. Compound 10e was found to be the most toxic compound to Ae. albopictus and Cx. quinquefasciatus. The LC50 of 10e against Ae. albopictus was found to be 6.42 and 5.25 mg/L at 24 and 48 h, respectively, whereas it was 7.01 and 3.88 mg/L, respectively in Cx. quinquefasciatus. Temephos was used as positive control. Copyright © 2014 Elsevier Ltd. All rights reserved.

Anchoring of Cu(II) onto surface of porous metal-organic framework through post-synthesis modification for the synthesis of benzimidazoles and benzothiazoles

Science.gov (United States)

Kardanpour, Reihaneh; Tangestaninejad, Shahram; Mirkhani, Valiollah; Moghadam, Majid; Mohammadpoor-Baltork, Iraj; Zadehahmadi, Farnaz

2016-03-01

Efficient synthesis of various benzimidazoles and benzothiazoles under mild conditions catalyzed by Cu(II) anchored onto UiO-66-NH2 metal organic framework is reported. In this manner, first, the aminated UiO-66 was modified with thiophene-2-carbaldehyde and then the prepared Schiff base was reacted with CuCl2. The prepared catalyst was characterized by FT-IR, UV-vis, X-ray diffraction (XRD), X-ray photoelectron spectroscopy (XPS), N2 adsorption, inductively coupled plasma atomic emission spectroscopy (ICP-AES) and field emission scanning electron microscopy (FE-SEM). The UiO-66-NH2-TC-Cu was applied as a highly efficient catalyst for synthesis of benzimidazole and benzothiazole derivatives by the reaction of aldehydes with 1,2-diaminobenzene or 2-aminothiophenol. The Cu(II)-containing MOF was reused several times without any appreciable loss of its efficiency.

How Jupiter's Ring Was Discovered.

Science.gov (United States)

Elliot, James; Kerr, Richard

1985-01-01

"Rings" (by astronomer James Elliot and science writer Richard Kerr) is a nontechnical book about the discovery and exploration of ring systems from the time of Galileo to the era of the Voyager spacecraft. One of this book's chapters is presented. (JN)

The Lord of Rings - the mysterious case of the stolen rings: a critical analysis

Science.gov (United States)

Sandrelli, S.

The Lord of Rings - the mysterious case of the stolen rings: a critical analysis S. Sandrelli INAF - Osservatorio Astronomico di Brera, Milano, Italy (stefano.sandrelli@brera.inaf.it / Fax: 02 72001600 / Phone: +39 02 72320337) "The Lord of Rings - the mysterious case of the stolen rings" is a live astronomical role-playing game for kids aged 10 -13. Its goal is to introduce them to some of the main topics of the Solar System: a) the role of gravity; b) the distribution of mass & light; c) the effects of rotation; d) the distribution of water. The game was held both at the Perugia (2004) and the Genova Science Festival (2005), obtaining great success. Teams of about 6-8 members are introduced to Mr Schioppanelli, the astro-detective of the town (the name is a pun: it reminds Schiaparelli, the famous italian astronomer, and it is a slang expression meaning "ring-breaker"). Mr Schioppanelli has his office in an "gastronomical astronomical observatory", known as The Red Giant Pizzeria. Schioppanelli informs the kids that a mysterious Centaur succeded in stealing the rings of Saturn. The partecipants are appointed astro-detectives in-charge and asked to find the rings by browsing around the Solar System, which is scaled so as to fit the town historical centre or a pedestrian area, going from the Sun to Saturn or beyond, depending on the actual area at disposal. Great care must be taken allowing children playing only in a car-free area of the town. At the right scaled distances, the partecipants meet characters playing as the various planets. The kids can talk to them after solving a riddle, obtaining useful informations. A special characters play as a comet, timely going in and out of the inner solar system. The teams can also talk to some shepherd-moons of the rings. They easily discover that the rings were totally destroyed by the Centaur: a real disaster! They are also suggested to gather the necessary ingredients (gravity, light, rotation, inclination, dust and

Magnet power supply system for the ALS storage ring and booster

International Nuclear Information System (INIS)

Jackson, L.T.; Luchini, K.; Lutz, I.

1993-05-01

The Magnet Power Supply System is described by specification, design, hardware, and operating experience. A unique system for the one Hz, 1.5 GeV Booster, where the wideband QF and QD power supplies track the dipole current to within 0.1% at injection will be detailed. AC distribution system considerations related to inverting the stored energy of the booster magnet back into power grid will be discussed. The rational for linear correctors and individual quad supplies (225 total units) will be placed within the context of the storage-ring requirements

Structure of eight molecular salts assembled from noncovalent bonding between carboxylic acids, imidazole, and benzimidazole

Science.gov (United States)

Jin, Shouwen; Zhang, Huan; Liu, Hui; Wen, Xianhong; Li, Minghui; Wang, Daqi

2015-09-01

Eight organic salts of imidazole/benzimidazole have been prepared with carboxylic acids as 2-methyl-2-phenoxypropanoic acid, α-ketoglutaric acid, 5-nitrosalicylic acid, isophthalic acid, 4-nitro-phthalic acid, and 3,5-dinitrosalicylic acid. The eight crystalline forms reported are proton-transfer compounds of which the crystals and compounds were characterized by X-ray diffraction analysis, IR, mp, and elemental analysis. These structures adopted hetero supramolecular synthons, with the most common R22(7) motif observed at salts 2, 3, 5, 6 and 8. Analysis of the crystal packing of 1-8 suggests that there are extensive strong Nsbnd H⋯O, and Osbnd H⋯O hydrogen bonds (charge assisted or neutral) between acid and imidazolyl components in all of the salts. Except the classical hydrogen bonding interactions, the secondary propagating interactions also play important roles in structure extension. This variety, coupled with the varying geometries and number of acidic groups of the acids utilized, has led to the creation of eight supramolecular arrays with 1D-3D structure. The role of weak and strong noncovalent interactions in the crystal packing is analyzed. The results presented herein indicate that the strength and directionality of the Nsbnd H⋯O, and Osbnd H⋯O hydrogen bonds between acids and imidazole/benzimidazole are sufficient to bring about the formation of organic salts.

A Benzimidazole Proton Pump Inhibitor Increases Growth and Tolerance to Salt Stress in Tomato

Directory of Open Access Journals (Sweden)

Michael J. Van Oosten

2017-07-01

Full Text Available Pre-treatment of tomato plants with micromolar concentrations of omeprazole (OP, a benzimidazole proton pump inhibitor in mammalian systems, improves plant growth in terms of fresh weight of shoot and roots by 49 and 55% and dry weight by 54 and 105% under salt stress conditions (200 mM NaCl, respectively. Assessment of gas exchange, ion distribution, and gene expression profile in different organs strongly indicates that OP interferes with key components of the stress adaptation machinery, including hormonal control of root development (improving length and branching, protection of the photosynthetic system (improving quantum yield of photosystem II and regulation of ion homeostasis (improving the K+:Na+ ratio in leaves and roots. To our knowledge OP is one of the few known molecules that at micromolar concentrations manifests a dual function as growth enhancer and salt stress protectant. Therefore, OP can be used as new inducer of stress tolerance to better understand molecular and physiological stress adaptation paths in plants and to design new products to improve crop performance under suboptimal growth conditions.Highlight: Omeprazole enhances growth of tomato and increases tolerance to salinity stress through alterations of gene expression and ion uptake and transport.

Structural investigation of HIV-1 nonnucleoside reverse transcriptase inhibitors: 2-Aryl-substituted benzimidazoles

Science.gov (United States)

Ziółkowska, Natasza E.; Michejda, Christopher J.; Bujacz, Grzegorz D.

2009-11-01

Acquired immunodeficiency syndrome (AIDS) caused by the human immunodeficiency virus (HIV) is one of the most destructive epidemics in history. Inhibitors of HIV enzymes are the main targets to develop drugs against that disease. Nonnucleoside reverse transcriptase inhibitors of HIV-1 (NNRTIs) are potentially effective and nontoxic. Structural studies provide information necessary to design more active compounds. The crystal structures of four NNRTI derivatives of 2-aryl-substituted N-benzyl-benzimidazole are presented here. Analysis of the geometrical parameters shows that the structures of the investigated inhibitors are rigid. The important geometrical parameter is the dihedral angle between the planes of the π-electron systems of the benzymidazole and benzyl moieties. The values of these dihedral angles are in a narrow range for all investigated inhibitors. There is no significant difference between the structure of the free inhibitor and the inhibitor in the complex with RT HIV-1. X-ray structures of the investigated inhibitors are a good basis for modeling enzyme-inhibitor interactions in rational drug design.

Magnetization of two coupled rings

International Nuclear Information System (INIS)

Avishai, Y; Luck, J M

2009-01-01

We investigate the persistent currents and magnetization of a mesoscopic system consisting of two clean metallic rings sharing a single contact point in a magnetic field. Many novel features with respect to the single-ring geometry are underlined, including the explicit dependence of wavefunctions on the Aharonov-Bohm fluxes, the complex pattern of two-fold and three-fold degeneracies, the key role of length and flux commensurability, and in the case of commensurate ring lengths the occurrence of idle levels which do not carry any current. Spin-orbit interactions, induced by the electric fields of charged wires threading the rings, give rise to a peculiar version of the Aharonov-Casher effect where, unlike for a single ring, spin is not conserved. Remarkably enough, this can only be realized when the Aharonov-Bohm fluxes in both rings are neither integer nor half-integer multiples of the flux quantum

Infrared cavity ring-down spectroscopy with a CW diode laser system

NARCIS (Netherlands)

Hemerik, M.M.; Kroesen, G.M.W.; Doebele, H.F.; Muraoka, K.

1999-01-01

We report on the first measurements with our CRDS setup. Although the diode laser system was out of order, we were able to test the most important parts with the use of a CO laser. The first results show a ring-down time of 1.54 ~is, which is in perfect agreement with the predicted reflectivity of

Preparation and evaluation of some benzimidazole derivatives as antioxidants for local base oil

Directory of Open Access Journals (Sweden)

J.S. Basta

2017-12-01

Full Text Available Some benzimidazole derivatives, 2(1-H benzo(dimidazole-2-y1thio N-butyl acetamide Ia, 2(I-H benzo(dimidazole-2-ylthio N-octylacetamid Ib and 2(I-H benzo(dimidazole-2-yl thio N-dodecylactamide Ic were prepared and studied as antioxidants for base stock. The structure of these compounds was elucidated by elemental analysis, IR and 1H NMR spectroscopy. The inhibition efficiency of the prepared compounds was determined by studying the oxidation stability of the local base oil via the change in total acid number (TAN, viscosity and infrared (IR spectroscopy.

Report of the eRHIC Ring-Ring Working Group

Energy Technology Data Exchange (ETDEWEB)

Aschenauer, E. C. [Brookhaven National Lab. (BNL), Upton, NY (United States); Berg, S. [Brookhaven National Lab. (BNL), Upton, NY (United States); Blaskiewicz, M. [Brookhaven National Lab. (BNL), Upton, NY (United States); Brennan, M. [Brookhaven National Lab. (BNL), Upton, NY (United States); Fedotov, A. [Brookhaven National Lab. (BNL), Upton, NY (United States); Fischer, W. [Brookhaven National Lab. (BNL), Upton, NY (United States); Litvinenko, V. [Brookhaven National Lab. (BNL), Upton, NY (United States); Montag, C. [Brookhaven National Lab. (BNL), Upton, NY (United States); Palmer, R. [Brookhaven National Lab. (BNL), Upton, NY (United States); Parker, B. [Brookhaven National Lab. (BNL), Upton, NY (United States); Peggs, S. [Brookhaven National Lab. (BNL), Upton, NY (United States); Ptitsyn, V. [Brookhaven National Lab. (BNL), Upton, NY (United States); Ranjbar, V. [Brookhaven National Lab. (BNL), Upton, NY (United States); Tepikian, S. [Brookhaven National Lab. (BNL), Upton, NY (United States); Trbojevic, D. [Brookhaven National Lab. (BNL), Upton, NY (United States); Willeke, F. [Brookhaven National Lab. (BNL), Upton, NY (United States)

2015-10-13

This report evaluates the ring-ring option for eRHIC as a lower risk alternative to the linac-ring option. The reduced risk goes along with a reduced initial luminosity performance. However, a luminosity upgrade path is kept open. This upgrade path consists of two branches, with the ultimate upgrade being either a ring-ring or a linac-ring scheme. The linac-ring upgrade could be almost identical to the proposed linac-ring scheme, which is based on an ERL in the RHIC tunnel. This linac-ring version has been studied in great detail over the past ten years, and its significant risks are known. On the other hand, no detailed work on an ultimate performance ring-ring scenario has been performed yet, other than the development of a consistent parameter set. Pursuing the ring-ring upgrade path introduces high risks and requires significant design work that is beyond the scope of this report.

The simulation of control system for the KEK main ring power supply, 1

International Nuclear Information System (INIS)

Sato, Hikaru; Shintomi, Takakazu; Kubo, Tadashi; Masuda, Masayoshi; Nakano, Michio.

1975-09-01

The simulation of control system for the KEK main ring power supply is performed. The inductance of the magnet is assumed to be linear against to the current. The results of the simulations are described. (auth.)

Commissioning of the diamond light source storage ring vacuum system

International Nuclear Information System (INIS)

Cox, M P; Boussier, B; Bryan, S; Macdonald, B F; Shiers, H S

2008-01-01

The Diamond storage ring has been operating with a 3 GeV electron beam since September 2006 and 190 A.h of beam dose have been accumulated. The pressure in the storage ring is 4.2 10 -10 mbar without beam, rising to 7.9 10 -10 mbar with 125 mA of stored beam. Data on the storage ring vacuum performance and experience from commissioning and beam conditioning are presented

Characterization and reactions of a Salix extractive with a unique ring system

Science.gov (United States)

Lawrence Landucci; Sally Ralph; Kolby Hirth

2003-01-01

An extractive compound with a novel ring system was isolated from the wood of Salix alba and was given the name Salucci. The compound was primarily identified from the 1D NMR, 2D NMR and LC-MSMS data and the structure investigated through reactions and derivatizations.

Novel benzimidazole derivatives as phosphodiesterase 10A (PDE10A) inhibitors with improved metabolic stability.

Science.gov (United States)

Chino, Ayaka; Masuda, Naoyuki; Amano, Yasushi; Honbou, Kazuya; Mihara, Takuma; Yamazaki, Mayako; Tomishima, Masaki

2014-07-01

In this study, we report the identification of potent benzimidazoles as PDE10A inhibitors. We first identified imidazopyridine 1 as a high-throughput screening hit compound from an in-house library. Next, optimization of the imidazopyridine moiety to improve inhibitory activity gave imidazopyridinone 10b. Following further structure-activity relationship development by reducing lipophilicity and introducing substituents, we acquired 35, which exhibited both improved metabolic stability and reduced CYP3A4 time-dependent inhibition. Copyright © 2014. Published by Elsevier Ltd.

One-pot, two-step synthesis of imidazo[1,2-a]benzimidazoles via a multicomponent [4 + 1] cycloaddition reaction.

Science.gov (United States)

Hsiao, Ya-Shan; Narhe, Bharat D; Chang, Ying-Sheng; Sun, Chung-Ming

2013-10-14

A one-pot, two-step synthesis of imidazo[1,2-a]benzimidazoles has been achieved by a three-component reaction of 2-aminobenzimidazoles with an aromatic aldehyde and an isocyanide. The reaction involving condensation of 2-aminobenzimidazole with an aldehyde is run under microwave activation to generate an imine intermediate under basic conditions which then undergoes [4 + 1] cycloaddition with an isocyanide.

2-(2-Hydroxy-3-methoxyphenyl-1H-benzimidazol-3-ium perchlorate

Directory of Open Access Journals (Sweden)

Chuan Chen

2012-06-01

Full Text Available In the title molecular salt, C14H13N2O2+·ClO4−, the ring systems in the cation are almost coplanar [dihedral angle = 5.53 (13°]. Intramolecular N—H...O and O—H...O hydrogen bonds generate S(6 and S(5 rings, respectively. In the crystal, the two H atoms involved in the intramolecular hydrogen bonds also participate in intermolecular links to acceptor O atoms of the perchlorate anions. A simple intermolecular N—H...O bond also occurs. Together, these form a double-chain structure along [101].

Electronic de-multipliers II (ring-shape systems); Demultiplieurs electroniques II (systeme en anneau)

Energy Technology Data Exchange (ETDEWEB)

Raievski, V

1948-09-01

This report describes a new type of ring-shape fast electronic counter (de-multiplier) with a resolution capacity equivalent to the one made by Regener (Rev. of Scientific Instruments USA 1946, 17, 180-89) but requiring two-times less electronic valves. This report follows the general description of electronic de-multipliers made by J. Ailloud (CEA--001). The ring comprises 5 flip-flop circuits with two valves each. The different elements of the ring are calculated with enough details to allow the transfer of this calculation to different valve types. (J.S.)

Bonding and energy parameters for Pr and Nd complexes of benzimidazoles

Energy Technology Data Exchange (ETDEWEB)

Mittal, S; Vyas, P C; Oza, C K [Rajasthan Univ., Jaipur (India). Dept. of Chemistry

1991-01-01

Complexes of praseodymium(III) and neodymium(III) with benzimidazoles have been synthesized and characterized by their conductance and infrared spectral studies. The values of interelectronic repulsion, i.e. Slater-Condon (F{sub 2}, F{sub 4}, F{sub 6}), Racah (E{sup 1}, E{sup 2}, E{sup 3}) parameters and spin-orbit interaction referred as Lande' ({zeta}4f) parameters have been calculated from their electronic spectral data. A comparison of these parameters for the complexes with Pr{sup 3+} and Nd{sup 3+} free ion parameters is discussed. Using F{sub 2} values, the nephelauxetic ratio({Beta}) and bonding parameter(b{sup 1/2}) have beeen calculated. The relative variation of covalent bonding in the complexes has been reported. (author). 11 refs., 1 tab.

Estimation of the cost of large-scale school deworming programmes with benzimidazoles.

Science.gov (United States)

Montresor, A; Gabrielli, A F; Diarra, A; Engels, D

2010-02-01

This study estimates the cost of distributing benzimidazole tablets in the context of school deworming programmes: we analysed studies reporting the cost of school deworming from seven countries in four WHO regions. The estimated cost for drug procurement to cover one million children (including customs clearance and international transport) is approximately US$20000. The estimated financial costs (including the cost of training of personnel, drug transport, social mobilization and monitoring) is, on average, equivalent to US$33000 per million school-age children with minimal variation in different countries and continents. The estimated economic costs of distribution (including the time spent by teachers, and health personnel at central, provincial and district level) to cover one million children approximately corresponds to US$19000. This study shows the minimal cost of school deworming activities, but also shows the significant contribution (corresponding to a quarter of the entire cost of the programme) provided by health and education systems in endemic countries even in the case of drug donations and donor support of distribution costs. Copyright 2009 Royal Society of Tropical Medicine and Hygiene. Published by Elsevier Ltd. All rights reserved.

Ring-Expansion/Contraction Radical Crossover Reactions of Cyclic Alkoxyamines: A Mechanism for Ring Expansion-Controlled Radical Polymerization

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Atsushi Narumi

2018-06-01

Full Text Available Macrocyclic polymers present an important class of macromolecules, displaying the reduced radius of gyration or impossibility to entangle. A rare approach for their synthesis is the ring expansion-controlled radical “vinyl” polymerization, starting from a cyclic alkoxyamine. We here describe ring-expansion radical crossover reactions of cyclic alkoxyamines which run in parallel to chain-propagation reactions in the polymerization system. The radical crossover reactions extensively occurred at 105–125 °C, eventually producing high molecular weight polymers with multiple inherent dynamic covalent bonds (NOC bonds. A subsequent ring-contraction radical crossover reaction and the second ring-expansion radical crossover reaction are also described. The major products for the respective three stages were shown to possess cyclic morphologies by the molecular weight profiles and the residual ratios for the NOC bonds (φ in %. In particular, the high φ values ranging from ca. 80% to 98% were achieved for this cyclic alkoxyamine system. This result verifies the high availability of this system as a tool demonstrating the ring-expansion “vinyl” polymerization that allows them to produce macrocyclic polymers via a one-step vinyl polymerization.

Mechanism of the pharmacokinetic interaction between methotrexate and benzimidazoles: potential role for breast cancer resistance protein in clinical drug-drug interactions

NARCIS (Netherlands)

Breedveld, Pauline; Zelcer, Noam; Pluim, Dick; Sönmezer, Ozgür; Tibben, Matthijs M.; Beijnen, Jos H.; Schinkel, Alfred H.; van Tellingen, Olaf; Borst, Piet; Schellens, Jan H. M.

2004-01-01

The antifolate drug methotrexate (MTX) is transported by breast cancer resistance protein (BCRP; ABCG2) and multidrug resistance-associated protein1-4 (MRP1-4; ABCC1-4). In cancer patients, coadministration of benzimidazoles and MTX can result in profound MTX-induced toxicity coinciding with an

INJECTION EFFICIENCY IN COMPTON RING NESTOR

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P. I. Gladkikh

2017-12-01

Full Text Available NESTOR is the hard X-ray source that is under commissioning at NSC KIPT. NESTOR based on the Compton scattering of laser photons on relativistic electrons. The structure of the facility can be represented as the following components: a linear accelerator, a transport channel, a storage ring, and a laser-optical system. Electrons are stored in the storage ring for energy of 40-200 MeV. Inevitable alignment errors of magnetic elements are strongly effect on the beam dynamics in the storage ring. These errors lead to a shift of the equilibrium orbit relative to the ideal one. Significant shift of the equilibrium orbit could lead to loss of the beam on physical apertures. Transverse sizes of electron and laser beams are only few tens of microns at the interaction point. The shift of electron beam at the interaction point could greatly complicate the operation adjustment of storage ring without sufficient beam position diagnostic system. This article presents the simulation results of the efficiency of electron beam accumulation in the NESTOR storage ring. Also, this article is devoted to electron beam dynamics due to alignment errors of magnetic element in the ring.

Testing reachability and stabilizability of systems over polynomial rings using Gröbner bases

NARCIS (Netherlands)

Habets, L.C.G.J.M.

1993-01-01

Conditions for the reachability and stabilizability of systems over polynomial rings are well-known in the literature. For a system $ \\Sigma = (A,B)$ they can be expressed as right-invertibility cconditions on the matrix $(zI - A \\mid B)$. Therefore there is quite a strong algebraic relationship

Storage ring development at the National Synchrotron Light Source

International Nuclear Information System (INIS)

Krinsky, S.; Bittner, J.; Fauchet, A.M.; Johnson, E.D.; Keane, J.; Murphy, J.; Nawrocky, R.J.; Rogers, J.; Singh, O.V.; Yu, L.H.

1991-09-01

This report contains papers on the following topics: Transverse Beam Profile Monitor; Bunch Length Measurements in the VUV Storage Ring; Photoelectric Effect Photon Beam Position Monitors; RF Receivers for Processing Electron Beam Pick-up Electrode Signals; Real-Time Global Orbit Feedback Systems; Local Orbit Feedback; Active Interlock System for High Power Insertion Devices in the X-ray Ring; Bunch Lengthening Cavity for the VUV Ring; SXLS Storage Ring Design

Galactic rings revisited - I. CVRHS classifications of 3962 ringed galaxies from the Galaxy Zoo 2 Database

Science.gov (United States)

Buta, Ronald J.

2017-11-01

Rings are important and characteristic features of disc-shaped galaxies. This paper is the first in a series that re-visits galactic rings with the goals of further understanding the nature of the features and for examining their role in the secular evolution of galaxy structure. The series begins with a new sample of 3962 galaxies drawn from the Galaxy Zoo 2 citizen science data base, selected because zoo volunteers recognized a ring-shaped pattern in the morphology as seen in Sloan Digital Sky Survey colour images. The galaxies are classified within the framework of the Comprehensive de Vaucouleurs revised Hubble-Sandage system. It is found that zoo volunteers cued on the same kinds of ring-like features that were recognized in the 1995 Catalogue of Southern Ringed Galaxies. This paper presents the full catalogue of morphological classifications, comparisons with other sources of classifications and some histograms designed mainly to highlight the content of the catalogue. The advantages of the sample are its large size and the generally good quality of the images; the main disadvantage is the low physical resolution that limits the detectability of linearly small rings such as nuclear rings. The catalogue includes mainly inner and outer disc rings and lenses. Cataclysmic (`encounter-driven') rings (such as ring and polar ring galaxies) are recognized in less than 1 per cent of the sample.

Antibacterial activity of cobalt(II complexes with some benzimidazole derivatives

Directory of Open Access Journals (Sweden)

S. O. PODUNAVAC-KUZMANOVIC

2008-12-01

Full Text Available The antibacterial activities of cobalt(II complexes with two series of benzimidazoles were evaluated in vitro against three Gram-positive bacterial strains (Bacillus cereus, Staphylococcus aureus, and Sarcina lutea and one Gram-negative isolate (Pseudomonas aeruginosa. The minimum inhibitory concentration was determined for all the complexes. The majority of the investtigated complexes displayed in vitro inhibitory activity against very persistent bacteria. They were found to be more active against Gram-positive than Gram-negative bacteria. It may be concluded that the antibacterial activity of the compounds is related to the cell wall structure of the tested bacteria. Comparing the inhibitory activities of the tested complexes, it was found that the 1-substituted-2-aminobenzimidazole derivatives were more active than complexes of 1-substituted-2-amino-5,6-dimethylbenzimidazoles. The effect of chemical structure on the antibacterial activity is discussed.

Developments in Geometric Metadata and Tools at the PDS Ring-Moon Systems Node

Science.gov (United States)

Showalter, M. R.; Ballard, L.; French, R. S.; Gordon, M. K.; Tiscareno, M. S.

2018-04-01

Object-Oriented Python/SPICE (OOPS) is an overlay on the SPICE toolkit that vastly simplifies and speeds up geometry calculations for planetary data products. This toolkit is the basis for much of the development at the PDS Ring-Moon Systems Node.

Monitor and control systems for the SLD Cherenkov Ring Imaging Detector

International Nuclear Information System (INIS)

Antilogus, P.; Aston, D.; Bienz, T.; Boston Univ., MA; California Univ., Santa Barbara, CA; California Univ., Santa Cruz, CA; Cincinnati Univ., OH; Rutgers--the State Univ., Piscataway, NJ; Tohoku Univ., Sendai

1989-10-01

To help ensure the stable long-term operation of a Cherenkov Ring Detector at high efficiency, a comprehensive monitor and control system is being developed. This system will continuously monitor and maintain the correct operating temperatures, and will provide an on-line monitor and maintain the correct operating temperatures, and will provide an on-line monitor of the pressures, flows, mixing, and purity of the various fluids. In addition the velocities and trajectories of Cherenkov photoelectrons drifting within the imaging chambers will be measured using a pulsed uv lamp and a fiberoptic light injection system. 9 refs., 6 figs

Comparison of cold and warm vacuum systems for intersecting storage rings

International Nuclear Information System (INIS)

Halama, H.J.; Herrera, J.C.

1975-01-01

In storage rings employing superconducting magnets, the use of a cold bore as a cryopump appears, at first glance, as simple and economical. Since the selection of a cold or warm vacuum system has far-reaching implications on the basic design, each system is considered in some detail. The theoretical and practical limitations imposed on the maximum beam current by the gas desorption from the chamber walls are discussed. A realistic design of a cold vacuum chamber is developed and then compared with the proposed warm ISABELLE vacuum system. The comparison shows that the warm approach is preferable. (U.S.)

99mTc labeled benzimidazole for detecting brain application

International Nuclear Information System (INIS)

Kumar, Nitin; Srivastava, V.; Tiwari, A.K.; Mishra, A.K.

2010-01-01

Full text: The synthesis and structure-activity relationship of a new class of Benzimidazole/Benzthiazole derivatives with low-nanomolar affinity for the Dopaminergic catachol and high selectivity versus the MAO receptor were found. Based on their chemical structure, four new derivatives which contain atoms to afford future labeling with PET isotopes, were synthesized and evaluated for enzyme activity. All the compound were tested for radiopharmaceutical efficacy. The % radiolabeling efficacy were found more than 95% after 24 hrs. The blood kinetics were found fast in nature which shows that this drug can be utilized for such application in which drug will go in longer time. The % reach in brain were found 3 to 5% which confirms that it can be utilized as brain imaging agent. The Enzyme kinetics of this compound has been studied spectrophotometrically at 25.0 deg C and at constant ionic strength of 0.10 mol dm-3. The products were identified by LCESI-MS technique and other spectral studies

Possible origin of Saturn's newly discovered outer ring

International Nuclear Information System (INIS)

Moehlmann, D.

1986-01-01

Within a planetogonic model the self-gravitationally caused formation of pre-planetary and pre-satellite rings from an earlier thin disk is reported. The theoretically derived orbital radii of these rings are compared with the orbital levels in the planetary system and the satellite systems of Jupiter, Saturn and Uranus. From this comparison it is concluded that at the radial position of Saturn's newly discovered outer ring an early pre-satellite ring of more or less evolved satellites could have existed. These satellites should have been disturbed in their evolution by the gravitation of the neighbouring massive satellite Titan. The comparison also may indicate similarities between the asteroidal belt and the newly discovered outer ring of Saturn

Outcome after Discontinuing Long-Term Benzimidazole Treatment in 11 Patients with Non-resectable Alveolar Echinococcosis with Negative FDG-PET/CT and Anti-EmII/3-10 Serology

Science.gov (United States)

Stumpe, Katrin D. M.; Grimm, Felix; Deplazes, Peter; Huber, Sabine; Bertogg, Kaja; Fischer, Dorothee R.; Müllhaupt, Beat

2015-01-01

Background/Aims Benzimidazoles are efficacious for treating non-resectable alveolar echinococcosis (AE), but their long-term parasitocidal (curative) effect is disputed. In this study, we prospectively analyzed the potential parasitocidal effect of benzimidazoles and whether normalization of FDG-PET/CT scans and anti-Emll/3-10-antibody levels could act as reliable "in vivo" parameters of AE-inactivation permitting to abrogate chemotherapy with a low risk for AE-recurrence. Method This prospective study included 34 patients with non-resectable AE subdivided into group A (n = 11), followed-up after diagnosis and begin of chemotherapy at months 6, 12 and 24, and group B (n = 23) with a medium duration of chemotherapy of 10 (range 2–25) years. All patients were assessed by FDG-PET/CT examinations and anti-EmII/3-10 serology. Chemotherapy was abrogated in patients with normalization of FDG-PET/CT and serum anti-EmII/3-10 levels. These patients were closely followed-up for AE recurrence. Endpoint (parasitocidal efficacy) was defined by the absence of AE-recurrence >24 months after stopping treatment. Results Normalization of FDG-PET/CT scan and anti-EmII/3-10 levels occurred in 11 of 34 patients (32%). After abrogation of chemotherapy in these 11 patients, there was no evidence of AE-recurrence within a median of 70.5 (range 16–82) months. However, the patients’ immunocompetence appears pivotal for the described long-term parasitocidal effect of benzimidazoles. Conclusions The combination of negative FDG-PET/CT-scans and anti-EmII/3-10 antibody levels seem to be reliable parameters for assessing in vivo AE-larval inactivity after long-term benzimidazole chemotherapy. Trial Registration clinicaltrials.gov: NCT00658294 PMID:26389799

The Saturnian rings

International Nuclear Information System (INIS)

Alfven, H.

1975-09-01

The structure of the Saturnian rings is traditionally believed to be due to resonances caused by Mimas (and possibly other satellites). It is shown that both theoretical and observational evidence rule out this interpretation. The increased observational accuracy on one hand and the increased understanding of the cosmogonic processes on the other makes it possible to explain the structure of the ring system as a product of condensation from a partially corotating plasma. In certain respects the agreement between theory and observations is about 1%. (Auth.)

Comparative plasma disposition kinetics of albendazole and its new benzimidazol prodrug in dog.

Science.gov (United States)

Khalil, Z; El Karbane, M; Faouzi, M E A; Ansar, M; Azougagh, M; El Harti, J; Taoufik, J

2016-01-01

The comparative pharmacokinetic behavior of albendazole (ABZ) and its new benzimidazol prodrug [1-tert-butyloxycarbonyl-5-propylthio-1-H-benzimidazol-2ylcarbamate of methyl] (ABZBoc), following their oral administration (10mg/kg) to healthy dogs was explored. Blood samples were obtained serially over a 24h period after treatment, then the plasma was analyzed by high-performance liquid chromatography (HPLC) to search the albendazole metabolites (ABZSO and ABZSO2). However, the albendazole parent drug was not detectable at any time after both treatments (ABZ and ABZBoc). By albendazole metabolites (ABZSO and ABZSO2) were the analytes recovered in the plasma after oral administration of ABZ and ABZBoc. Furthermore, some amounts of ABZBoc were also available in the plasma samples treated with this new produg. The plasma profile of each analyte followed a similar pattern after both treatments, the active metabolite (ABZSO) was the major analyte recovered in plasma (between 1 and 24h post-treatment). The pharmacokinetic parameters of both groups were calculated (Cmax, Tmax, t1/2, AUC0-›∞), and analyzed using the Student's t-test, Palbendazole metabolites (ABZSO, ABZSO2) between the group treated with albendazole (group A) and that treated with ABZBoc prodrug (group B). Hence, the levels of the various pharmacokinetics parameters were low in the group treated with prodrug, as well they did not reach equivalent concentrations to that of albendazole. These differences between albendazole and its new prodrug may be explained by the fact that ABZBoc prodrug was not effectively reduced in the intestine of dogs. Copyright © 2015 Académie Nationale de Pharmacie. Published by Elsevier Masson SAS. All rights reserved.

Spectral characteristics of 2-(4'-amino-3-pyridyl)benzimidazole: Effects of solvent and acid or base concentration

International Nuclear Information System (INIS)

Dogra, Sneh K.

2006-01-01

Spectral characteristics of 2-(4'-amino-3-pyridyl)benzimidazole (4-A3PyBI) have been studied in different solvents, as well as at different acid or base concentrations using absorption, fluorescence excitation and fluorescence spectroscopy. Excited singlet state (S 1 ) lifetimes for each species were measured using nanosecond time-dependent spectrofluorimeter. AM1 semi-empirical and density functional theoretical (DFT) calculations were performed on each species for the spectral assignment. From the above results it is concluded that 4-A3PyBI exists only in the amine form. First protonation occurs at pyridine=N- atom and second protonation at the benzimidazole (BI)=N- atom. When dication (DC) species is excited, two emission bands are observed, having the same fluorescence excitation spectra, suggesting the same ground state (S ) precursor. Short wavelength (SW) emission band is assigned to the π-π* transition and long wavelength (LW) emission to the charge transfer transition. First deprotonation in S state occurs from >N-H moiety, whereas in S 1 state it is from -NH 2 group. Monoanion (MA) so formed in S 1 state is non-fluorescent. Dianion (DA) is formed by further deprotonating >N-H moiety in S 1 state and it is fluorescent. pK a values were determined and discussed

ASSOCIATIVE RINGS SOLVED AS LIE RINGS

Directory of Open Access Journals (Sweden)

M. B. Smirnov

2011-01-01

Full Text Available The paper has proved that an associative ring which is solvable of a n- class as a Lie ring has a nilpotent ideal of the nilpotent class not more than 3×10n–2  and a corresponding quotient ring satisfies an identity [[x1, x2, [x3, x4

Control of ring lasers by means of coupled cavities

DEFF Research Database (Denmark)

Buchhave, Preben; Abitan, Haim; Tidemand-Lichtenberg, Peter

2000-01-01

Variable phase coupling to an external ring is used to control a unidirectional ring laser. The observed behavior of the coupled rings is explained theoretically. We have found experimentally that by quickly changing the phase of the feedback from the external ring it is possible to Q......-switch the ring laser. Also, at certain values of the phase of the feedback in the external ring, instabilities in the total system occur and oscillations arise in the ring laser....

The terminal Eocene event - Formation of a ring system around the earth

Science.gov (United States)

Okeefe, J. A.

1980-01-01

It is suggested that the formation of a ring system about the earth by particles and debris related to the North American strewn tektite field is responsible for the terminal Eocene event of 34 million years ago, in which severe climatic changes accompanied by widespread biological extinctions occurred. Botanical data is cited which implies a 20-C decrease in winter temperature with no change in summer temperature, and evidence of the correlation of the North American tektite fall, which is estimated to have a total mass of 10 to the 9th to 10 to the 10th tons, with the disappearance of five of the most abundant species of radiolaria is presented. The possible connection between the tektites and climatic change is argued to result from the screening of sunlight by an equatorial ring of trapped particles of extraterrestrial origin in geocentric orbit which would cut off sunlight only in the winter months. Such a ring, located at a distance of between 1.5 and 2.5 earth radii (the Roche limit) is estimated to have a lifetime of a few million years.

Non-Linear Dynamics of Saturn's Rings

Science.gov (United States)

Esposito, L. W.

2016-12-01

Non-linear processes can explain why Saturn's rings are so active and dynamic. Ring systems differ from simple linear systems in two significant ways: 1. They are systems of granular material: where particle-to-particle collisions dominate; thus a kinetic, not a fluid description needed. Stresses are strikingly inhomogeneous and fluctuations are large compared to equilibrium. 2. They are strongly forced by resonances: which drive a non-linear response, that push the system across thresholds that lead to persistent states. Some of this non-linearity is captured in a simple Predator-Prey Model: Periodic forcing from the moon causes streamline crowding; This damps the relative velocity. About a quarter phase later, the aggregates stir the system to higher relative velocity and the limit cycle repeats each orbit, with relative velocity ranging from nearly zero to a multiple of the orbit average. Summary of Halo Results: A predator-prey model for ring dynamics produces transient structures like `straw' that can explain the halo morphology and spectroscopy: Cyclic velocity changes cause perturbed regions to reach higher collision speeds at some orbital phases, which preferentially removes small regolith particles; surrounding particles diffuse back too slowly to erase the effect: this gives the halo morphology; this requires energetic collisions (v ≈ 10m/sec, with throw distances about 200km, implying objects of scale R ≈ 20km).Transform to Duffing Eqn : With the coordinate transformation, z = M2/3, the Predator-Prey equations can be combined to form a single second-order differential equation with harmonic resonance forcing.Ring dynamics and history implications: Moon-triggered clumping explains both small and large particles at resonances. We calculate the stationary size distribution using a cell-to-cell mapping procedure that converts the phase-plane trajectories to a Markov chain. Approximating it as an asymmetric random walk with reflecting boundaries

A novel magnetic core-shell nanocomposite Fe3O4@chitosan@ZnO for the green synthesis of 2-benzimidazoles

Science.gov (United States)

Tian, Fei; Niu, Libo; Chen, Bo; Gao, Xuejia; Lan, Xingwang; Huo, Li; Bai, Guoyi

2017-10-01

A novel magnetic core-shell nanocomposite Fe3O4@Chitosan@ZnO was successfully prepared by in situ chemical precipitation method. It has a clear core-shell structure with magnetic Fe3O4 (about 160 nm in diameter) as core, chitosan as the inner shell, and ZnO as the outer shell, as demonstrated by the transmission electron microscopy and the related elemental mapping. Moreover, this nanocomposite has high magnetization (43.6 emu g-1) so that it can be easily separated from the reaction mixture within 4 s by an external magnetic field. The introduction of the natural chitosan shell, instead of the conventional SiO2 shell, and its combination with the active ZnO ensures this novel nanocomposite green character and good catalytic performance in the synthesis of 2-benzimidazoles with moderate to excellent isolated yields at room temperature. Notably, it can be recycled seven times without appreciable loss of its initial catalytic activity, demonstrating its good stability and making it an attractive candidate for the green synthesis of 2-benzimidazoles. [Figure not available: see fulltext.

Simultaneous determination of nitroimidazoles, benzimidazoles, and chloramphenicol components in bovine milk by ultra-high performance liquid chromatography-tandem mass spectrometry.

Science.gov (United States)

Wang, Yuanyuan; Li, Xiaowei; Zhang, Zhiwen; Ding, Shuangyang; Jiang, Haiyang; Li, Jiancheng; Shen, Jianzhong; Xia, Xi

2016-02-01

A sensitive, confirmatory ultra-high performance liquid chromatography-tandem mass spectrometric method was developed and validated to detect 23 veterinary drugs and metabolites (nitroimidazoles, benzimidazoles, and chloramphenicol components) in bovine milk. Compounds of interest were sequentially extracted from milk with acetonitrile and basified acetonitrile using sodium chloride to induce liquid-liquid partition. The extract was purified on a mixed mode solid-phase extraction cartridge. Using rapid polarity switching in electrospray ionization, a single injection was capable of detecting both positively and negatively charged analytes in a 9 min chromatography run time. Recoveries based on matrix-matched calibrations and isotope labeled internal standards for milk ranged from 51.7% to 101.8%. The detection limits and quantitation limits of the analytical method were found to be within the range of 2-20 ng/kg and 5-50 ng/kg, respectively. The recommended method is simple, specific, and reliable for the routine monitoring of nitroimidazoles, benzimidazoles, and chloramphenicol components in bovine milk samples. Copyright © 2015 Elsevier Ltd. All rights reserved.

Atmospheric pressure microwave plasma system with ring waveguide

International Nuclear Information System (INIS)

Liu Liang; Zhang Guixin; Zhu Zhijie; Luo Chengmu

2007-01-01

Some scientists used waveguide as the cavity to produce a plasma jet, while large volume microwave plasma was relatively hard to get in atmospheric pressure. However, a few research institutes have already developed devices to generate large volume of atmospheric pressure microwave plasma, such as CYRANNUS and SLAN series, which can be widely applied. In this paper, present a microwave plasma system with ring waveguide to excite large volume of atmospheric pressure microwave plasma, plot curves on theoretical disruption electric field of some working gases, emulate the cavity through software, measure the power density to validate and show the appearance of microwave plasma. At present, large volume of argon and helium plasma have already been generated steadily by atmospheric pressure microwave plasma system. This research can build a theoretical basis of microwave plasma excitation under atmospheric pressure and will be useful in study of the device. (authors)

Energy spectra of quantum rings.

Science.gov (United States)

Fuhrer, A; Lüscher, S; Ihn, T; Heinzel, T; Ensslin, K; Wegscheider, W; Bichler, M

2001-10-25

Quantum mechanical experiments in ring geometries have long fascinated physicists. Open rings connected to leads, for example, allow the observation of the Aharonov-Bohm effect, one of the best examples of quantum mechanical phase coherence. The phase coherence of electrons travelling through a quantum dot embedded in one arm of an open ring has also been demonstrated. The energy spectra of closed rings have only recently been studied by optical spectroscopy. The prediction that they allow persistent current has been explored in various experiments. Here we report magnetotransport experiments on closed rings in the Coulomb blockade regime. Our experiments show that a microscopic understanding of energy levels, so far limited to few-electron quantum dots, can be extended to a many-electron system. A semiclassical interpretation of our results indicates that electron motion in the rings is governed by regular rather than chaotic motion, an unexplored regime in many-electron quantum dots. This opens a way to experiments where even more complex structures can be investigated at a quantum mechanical level.

Measuring the electron-ion ring parameters by bremsstrahlung

International Nuclear Information System (INIS)

Inkin, V.D.; Mozelev, A.A.; Sarantsev, V.P.

1982-01-01

A system is described for measuring the number of electrons and ions in the electron-ion rings of a collective heavy ion accelerator. The system operation is based on detecting gamma quanta of bremsstrahlung following the ring electron interaction with the nuclei of neutral atoms and ions at different stages of filling the ring with ions. The radiation detector is a scintillation block - a photomultiplier operating for counting with NaI(Tl) crystal sized 30x30 mm and ensuring the detection efficiency close to unity. The system apparatus is made in the CAMAC standard and rems on-line with the TRA/i miniature computer. The block-diagrams of the system and algorithm of data processing are presented. A conclusion is drawn that the results of measuring the ring parameters with the use of the diagnostics system described are in good agreement within the range of measuring errors with those obtained by means of the diagnostics system employing synchrotron radiation and induction sensors

Rings Research in the Next Decade

Science.gov (United States)

Burns, J. A.; Tiscareno, M. S.

2009-12-01

The study of planetary ring systems forms a key component of planetary science for several reasons: 1) The evolution and current states of planets and their satellites are affected in many ways by rings, while 2) conversely, properties of planets and moons and other solar system populations are revealed by their effects on rings; 3) highly structured and apparently delicate ring systems may be bellwethers, constraining various theories of the origin and evolution of their entire planetary system; and finally, 4) planetary rings provide an easily observable analogue to other astrophysical disk systems, enabling real “ground truth” results applicable to disks much more remote in space and/or time, including proto-planetary disks, circum-stellar disks, and even galaxies. Significant advances have been made in rings science in the past decade. The highest-priority rings research recommendations of the last Planetary Science Decadal Survey were to operate and extend the Cassini orbiter mission at Saturn; this has been done with tremendous success, accounting for much of the progress made on key science questions, as we will describe. Important progress in understanding the rings of Saturn and other planets has also come from Earth-based observational and theoretical work, again as prioritized by the last Decadal Survey. However, much important work remains to be done. At Saturn, the Cassini Solstice Mission must be brought to a successful completion. Priority should also be placed on sending spacecraft to Neptune and/or Uranus, now unvisited for more than 20 years. At Jupiter and Pluto, opportunities afforded by visiting spacecraft capable of studying rings should be exploited. On Earth, the need for continued research and analysis remains strong, including in-depth analysis of rings data already obtained, numerical and theoretical modeling work, laboratory analysis of materials and processes analogous to those found in the outer solar system, and continued Earth

2-(2-Pyridyl) Benzimidazole Analogs and their beta-Glucuronidase Inhibitory Activity

International Nuclear Information System (INIS)

Kamil, A.; Noureen, S.

2015-01-01

Synthesis of 2-(2-Pyridyl) benzimidazole analogs 1-11 have been carried out and evaluated for in vitro beta-glucuronidase inhibitory potential. The compounds 4 (IC/sub 50/ = 4.06 ± 0.34 meuM), 5 (IC/sub 50/ = 09.63 ± 0.81 meuM), 1 (IC/sub 50/ = 19.66 ± 0.44 meuM), 7 (IC/sub 50/ = 24.75 ± 0.25 meuM), 6 (IC/sub 50/ = 26.30 ± 1.37 meuM), and 3 (IC/sub 50/ = 32.11 ± 0.89 meuM), showed beta-glucuronidase inhibitory activity superior to the standard D-saccharic acid 1,4-lactone, with (IC/sub 50/ = 48.4 ± 1.25 meuM). Based on structure-activity relationship, we discover a new class of potent beta-glucuronidase inhibitors. (author)

Ground Movement in SSRL Ring

International Nuclear Information System (INIS)

Sunikumar, Nikita

2011-01-01

Users of the Stanford Synchrotron Radiation Lightsource (SSRL) are being affected by diurnal motion of the synchrotron's storage ring, which undergoes structural changes due to outdoor temperature fluctuations. In order to minimize the effects of diurnal temperature fluctuations, especially on the vertical motion of the ring floor, scientists at SSRL tried three approaches: painting the storage ring white, covering the asphalt in the middle of the ring with highly reflective Mylar and installing Mylar on a portion of the ring roof and walls. Vertical motion in the storage ring is measured by a Hydrostatic Leveling System (HLS), which calculates the relative height of water in a pipe that extends around the ring. The 24-hr amplitude of the floor motion was determined using spectral analysis of HLS data, and the ratio of this amplitude before and after each experiment was used to quantitatively determine the efficacy of each approach. The results of this analysis showed that the Mylar did not have any significant effect on floor motion, although the whitewash project did yield a reduction in overall HLS variation of 15 percent. However, further analysis showed that the reduction can largely be attributed to a few local changes rather than an overall reduction in floor motion around the ring. Future work will consist of identifying and selectively insulating these local regions in order to find the driving force behind diurnal floor motion in the storage ring.

Non-Linear Dynamics of Saturn’s Rings

Science.gov (United States)

Esposito, Larry W.

2015-11-01

Non-linear processes can explain why Saturn’s rings are so active and dynamic. Ring systems differ from simple linear systems in two significant ways: 1. They are systems of granular material: where particle-to-particle collisions dominate; thus a kinetic, not a fluid description needed. We find that stresses are strikingly inhomogeneous and fluctuations are large compared to equilibrium. 2. They are strongly forced by resonances: which drive a non-linear response, pushing the system across thresholds that lead to persistent states.Some of this non-linearity is captured in a simple Predator-Prey Model: Periodic forcing from the moon causes streamline crowding; This damps the relative velocity, and allows aggregates to grow. About a quarter phase later, the aggregates stir the system to higher relative velocity and the limit cycle repeats each orbit.Summary of Halo Results: A predator-prey model for ring dynamics produces transient structures like ‘straw’ that can explain the halo structure and spectroscopy: This requires energetic collisions (v ≈ 10m/sec, with throw distances about 200km, implying objects of scale R ≈ 20km).Transform to Duffing Eqn : With the coordinate transformation, z = M2/3, the Predator-Prey equations can be combined to form a single second-order differential equation with harmonic resonance forcing.Ring dynamics and history implications: Moon-triggered clumping at perturbed regions in Saturn’s rings creates both high velocity dispersion and large aggregates at these distances, explaining both small and large particles observed there. We calculate the stationary size distribution using a cell-to-cell mapping procedure that converts the phase-plane trajectories to a Markov chain. Approximating the Markov chain as an asymmetric random walk with reflecting boundaries allows us to determine the power law index from results of numerical simulations in the tidal environment surrounding Saturn. Aggregates can explain many dynamic aspects

RF-to-RF Characterization of a Phased Array Receive Antenna Steering System Using a Novel Ring Resonator-Based Integrated Photonic Beamformer

NARCIS (Netherlands)

Zhuang, L.; Burla, M.; Roeloffzen, C.G.H.; Meijerink, Arjan; Marpaung, D.A.I.; Khan, M.R.H.; van Etten, Wim; Leinse, Arne; Hoekman, M.; Heideman, Rene

2009-01-01

A novel ring resonator-based photonic beamformer has been developed for continuous and squint-free control of the reception angle of broadband phased array antenna systems. The core of the system is a ring resonator based optical beamforming network (OBFN) used for delay synchronization and coherent

Mapping Ring Particle Cooling across Saturn's Rings with Cassini CIRS

Science.gov (United States)

Brooks, Shawn M.; Spilker, L. J.; Edgington, S. G.; Pilorz, S. H.; Deau, E.

2010-10-01

Previous studies have shown that the rings' thermal inertia, a measure of their response to changes in the thermal environment, varies from ring to ring. Thermal inertia can provide insight into the physical structure of Saturn's ring particles and their regoliths. Low thermal inertia and quick temperature responses are suggestive of ring particles that have more porous or fluffy regoliths or that are riddled with cracks. Solid, coherent particles can be expected to have higher thermal inertias (Ferrari et al. 2005). Cassini's Composite Infrared Spectrometer has recorded millions of spectra of Saturn's rings since its arrival at Saturn in 2004 (personal communication, M. Segura). CIRS records far infrared radiation between 10 and 600 cm-1 (16.7 and 1000 µm) at focal plane 1 (FP1), which has a field of view of 3.9 mrad. Thermal emission from Saturn's rings peaks in this wavelength range. FP1 spectra can be used to infer ring temperatures. By tracking how ring temperatures vary, we can determine the thermal inertia of the rings. In this work we focus on CIRS observations of the shadowed portion of Saturn's rings. The thermal budget of the rings is dominated by the solar radiation absorbed by its constituent particles. When ring particles enter Saturn's shadow this source of energy is abruptly cut off. As a result, ring particles cool as they traverse Saturn's shadow. From these shadow observations we can create cooling curves at specific locations across the rings. We will show that the rings' cooling curves and thus their thermal inertia vary not only from ring to ring, but by location within the individual rings. This research was carried out at the Jet Propulsion Laboratory, California Institute of Technology, under contract with NASA. Copyright 2010 California Institute of Technology. Government sponsorship acknowledged.

MATLAB based beam orbit correction system of HLS storage ring

International Nuclear Information System (INIS)

Ding Shichuan; Liu Gongfa; Xuan Ke; Li Weimin; Wang Lin; Wang Jigang; Li Chuan; Bao Xun; Guo Weiqun

2006-01-01

The distortion of closed orbit usually causes much side effect which is harmful to synchrotron radiation source such as HLS, so it is necessary to correct the distortion of closed orbit. In this paper, the correction principle, development procedure and test of MATLAB based on beam orbit correction system of HLS storage ring are described. The correction system is consisted of the beam orbit measure system, corrector magnet system and the control system, and the beam orbit correction code based on MATLAB is working on the operation interface. The data of the beam orbit are analyzed and calculated firstly, and then the orbit is corrected by changing corrector strength via control system. The test shows that the distortion of closed orbit is from max 4.468 mm before correction to max 0.299 mm after correction as well as SDEV is from 2.986 mm to 0.087 mm. So the correction system reaches the design goal. (authors)

One-pot Synthesis of Benzimidazoles and Benzothiazoles in the Presence of Fe(HSO4)3 as a New and Efficient Oxidant

International Nuclear Information System (INIS)

Eshghi, Hossein; Rahimizadeh, Mohammad; Shiri, Ali; Sedaghat, Parisa

2012-01-01

A series of substituted benzimidazoles and benzothiazoles were prepared through the one-pot reaction of ο-phenylenediamine and ο-aminothiophenol with various aldehydes in the presence of ferric hydrogensulfate both in EtOH and water as solvent. The reactions proceed smoothly in excellent yield, high chemoselectivity and with an easy work-up

Eight supramolecular assemblies constructed from bis(benzimidazole) and organic acids through strong classical hydrogen bonding and weak noncovalent interactions

Science.gov (United States)

Jin, Shouwen; Wang, Daqi

2014-05-01

Eight crystalline organic acid-base adducts derived from alkane bridged bis(N-benzimidazole) and organic acids (2,4,6-trinitrophenol, p-nitrobenzoic acid, m-nitrobenzoic acid, 3,5-dinitrobenzoic acid, 5-sulfosalicylic acid and oxalic acid) were prepared and characterized by X-ray diffraction analysis, IR, mp, and elemental analysis. Of the eight compounds five are organic salts (1, 4, 6, 7 and 8) and the other three (2, 3, and 5) are cocrystals. In all of the adducts except 1 and 8, the ratio of the acid and the base is 2:1. All eight supramolecular assemblies involve extensive intermolecular classical hydrogen bonds as well as other noncovalent interactions. The role of weak and strong noncovalent interactions in the crystal packing is ascertained. These weak interactions combined, all the complexes displayed 3D framework structure. The results presented herein indicate that the strength and directionality of the classical N+-H⋯O-, O-H⋯O, and O-H⋯N hydrogen bonds (ionic or neutral) and other nonbonding associations between acids and ditopic benzimidazoles are sufficient to bring about the formation of cocrystals or organic salts.

A reachability test for systems over polynomial rings using Gröbner bases

NARCIS (Netherlands)

Habets, L.C.G.J.M.

1992-01-01

Conditions for the reachability of a system over a polynomial ring are well known in the literature. However, the verification of these conditions remained a difficult problem in general. Application of the Gröbner Basis method from constructive commutative algebra makes it possible to carry out

Ring Avulsion Injuries: A Systematic Review.

Science.gov (United States)

Bamba, Ravinder; Malhotra, Gautam; Bueno, Reuben A; Thayer, Wesley P; Shack, R Bruce

2018-01-01

Ring avulsion injuries can range from soft tissue injury to complete amputation. Grading systems have been developed to guide treatment, but there is controversy with high-grade injuries. Traditionally, advanced ring injuries have been treated with completion amputation, but there is evidence that severe ring injuries can be salvaged. The purpose of this systematic review was to pool the current published data on ring injuries. A systematic review of the English literature published from 1980 to 2015 in PubMed and MEDLINE databases was conducted to identify patients who underwent treatment for ring avulsion injuries. Twenty studies of ring avulsion injuries met the inclusion criteria. There were a total of 572 patients reported with ring avulsion injuries. The Urbaniak class breakdown was class I (54 patients), class II (204 patients), and class III (314 patients). The average total arc of motion (TAM) for patients with a class I injury was 201.25 (n = 40). The average 2-point discrimination was 5.6 (n = 10). The average TAM for patients with a class II injury undergoing microsurgical revascularization was 187.0 (n = 114), and the average 2-point discrimination was 8.3 (n = 40). The average TAM for patients with a class III injury undergoing microsurgical revascularization was 168.2 (n = 170), and the average 2-point discrimination was 10.5 (n = 97). Ring avulsion injuries are commonly classified with the Urbaniak class system. Outcomes are superior for class I and II injuries, and there are select class III injuries that can be treated with replantation. Shared decision making with patients is imperative to determine whether replantation is appropriate.

The Ring System of Saturn as Seen by Cassini-VIMS (Invited)

Science.gov (United States)

Filacchione, G.; Ciarniello, M.; Capaccioni, F.

2015-08-01

Since 2004 the Visual and Infrared Mapping Spectrometer (VIMS) aboard Cassini has acquired numerous hyperspectral mosaics in the 0.35-5.1 μm spectral range of Saturn's main rings in very different illumination and viewing geometries. These observations have allowed us to infer the ring particles physical properties and composition: water ice abundance is estimated through the 1.25-1.5-2.0 μm band depths, chromophores distribution is derived from visible spectral slopes while organic material is traced by the aliphatic compounds signature at 3.42 μm which appears stronger on CD and C ring than on A-B rings (Filacchione et al., 2014). Observed reflectance spectra are fitted with a spectrophotometric model based on Montecarlo ray-tracing with the scope to infer particles composition while disentangling photometric effects (caused by multiple scattering, opposition surge and forward scattering) which depend on illumination/viewing geometries. Spectral bond albedo for different regions of the rings has been best-fitted using Hapke's radiative transfer modeling (Ciarniello et al, 2011) by choosing different mixtures of water ice, tholin, and amorphous carbon particles populations. While tholin distribution seems to be fairly constant across the rings, the amorphous carbon appears anti-correlated with optical depth. Moreover, dark material contamination is less effective on densest regions, where the more intense rejuvenation processes occur, in agreement with the ballistic transport theory (Cuzzi and Estrada,1998). Finally, the 3.6 μm continuum peak wavelength is used to infer particles temperature, which is anti-correlated with the albedo and the optical depth (tau): low-albedo/low-tau C ring and CD have higher temperatures than A-B rings where albedo and tau are high. This trend matches direct temperature measurements by CIRS (Spilker et al., 2013).

Gold nanoparticles supported on titanium dioxide: an efficient catalyst for highly selective synthesis of benzoxazoles and benzimidazoles.

Science.gov (United States)

Tang, Lin; Guo, Xuefeng; Yang, Yu; Zha, Zhenggen; Wang, Zhiyong

2014-06-11

A highly efficient and selective reaction for the synthesis of 2-substituted benzoxazoles and benzimidazoles catalyzed by Au/TiO2 has been developed via two hydrogen-transfer processes. This reaction has a good tolerance to air and water, a wide substrate scope, and represents a new avenue for practical C-N and C-O bond formation. More importantly, no additional additives, oxidants and reductants are required for the reaction and the catalyst can be recovered and reused readily.

Transformation of Zwitterionic Pyridine Derivatives to a Spiro-Fused Ring System: Azoniabenzo[de]fluorine. Synthesis and Mechanistic Rationalization.

Science.gov (United States)

Palkó, Roberta; Egyed, Orsolya; Rokob, Tibor András; Bombicz, Petra; Riedl, Zsuzsanna; Hajós, György

2015-01-02

Reaction of aryl- and benzylsulfanopyridinium amidates bearing a methyl group in position 6 with 2 equiv of diphenylketene afforded a spiro-fused ring system: azoniabenzo[de]fluorine. By use of an excess amount of ketene, a distinct reaction was observed via which a 1H-pyrrolo[3,2-b]pyridin-2(3H)-one derivative was furnished. The structure of the tetracyclic spiro-fused ring system was unambiguously confirmed by X-ray diffraction, and its formation was rationalized by DFT calculations.

Determination of benzimidazole residues and their metabolites in raw milk using high performance liquid chromatography-diode array detection

Directory of Open Access Journals (Sweden)

Marija Denžić Lugomer

2017-01-01

Full Text Available A new analytical method using high performance liquid chromatography-diode array detector (HPLC-DAD was developed for the analysis of 18 benzimidazoles and their metabolites in milk. Samples were extracted with acetonitrile and n-hexane and purified by polymer cation exchange (PCX solid phase extraction cartridges. LC separation was performed on Xbridge C18 with gradient elution using acetonitrile and ammonium acetate buffer. The DAD detection was set at 298, 312, 254 and 290 nm. The method was validated according to the criteria of Commission Decision 2002/657/EC. The following validation parameters were set: accuracy (expressed as recovery 31.7-137.6 %, limit of decision (CCα 6.0-120.6 μg kg-1, detection capability (CCβ 6.1-120.8 μg kg-1, limit of detection (LOD 1-4 μg kg-1, limit of quantification (LOQ 4-18 μg kg-1, precision as CV 7.0-22.5 %, withinlaboratory reproducibility expressed as CV 8.8-30.6 %. Finally, the developed method was applied to the analysis of collected milk samples. A total of 50 milk samples was analysed for benzimidazole residues. All obtained concentrations for all compounds were below the LOQ values.

Reflective variable optical attenuators and fibre ring lasers for wavelength-division multiplexing systems

Science.gov (United States)

Liu, He Liang

Wavelength division multiplexing (WDM) optical fibre system is an important enabling technology to fulfill the demands for bandwidth in the modern information age. The main objective of this project is to study novel devices with the potential to enhance the performance of WDM systems. In particular, a novel reflective variable optical attenuator (RVOA) used for dynamic gain equalization (DGE) and fibre lasers based on an entirely new type of erbium-doped fibres with ultrawide tuning range were investigated theoretically and experimentally. We proposed a new type of RVOA device which could be potentially integrated with arrayed waveguide grating (AWG) to reduce the cost of DGE substantially. Initially, fibre-based RVOAs, fabricated with optical fibre components such as fibre coupler and Faraday rotator mirror, were investigated theoretically and experimentally. Larger attenuation range up to 22 dB was realized for fibre coupler-based ROVA with a Faraday rotator mirror and its polarization-dependent loss is about 0.5 dB. Then polymeric waveguide-based RVOAs were investigated theoretically and experimentally. Using an epoxy Novolak resin as core material and an UV-cured resin (Norland's NOA61) as cladding material, a polymeric waveguide RVOA was successfully fabricated. The dynamic 15 dB attenuation range was achieved and the PDL was less than 0.2 dB. The measured insertion loss of the polymeric waveguide RVOA was too large (about 18 dB) and was mainly induced by coupling loss, material loss and poor alignment. In the second part of the study, fibre ring lasers with continuous wavelength tuning over wide wavelength range and fibre ring lasers with discrete wavelength tuning were investigated. Tunable lasers are important devices in WDM systems because they could be employed as reserved sources and therefore avoiding the need to stock large inventory of lasers to cover the ITU-wavelength grid. In this project, erbium ions doped bismuth oxide glass fibres instead of

Co(II), Ni(II) and Cu(II) complexes of methyl-5-(Phenylthio) benzimidazole-2-carbamate: Molecular structures, spectral and DFT calculations

Science.gov (United States)

Mansour, Ahmed M.; El Bakry, Eslam M.; Abdel-Ghani, Nour T.

2016-05-01

[Co(FBZ)2(H2O)]·2NO3·0.5H2O (1), [Ni(FBZ)2X2]·zH2O (X = Cl​-, z = 0.5 (2) and X = CH3COO-, z = 1 (3)) and [Cu(FBZ)2(H2O) (NO3)]·NO3·1.5H2O (4) (FBZ = methyl-5-(Phenylthio) benzimidazole-2-carbamate; Fenbendazole) complexes were synthesized and characterized by elemental analysis, thermal, IR, EPR, UV-Vis, magnetic and conductance measurements. Geometry optimization, molecular electrostatic potential maps and natural bond orbital analysis were carried out at DFT/B3LYP/6-31G∗ level of theory. FBZ behaves as a neutral bidentate ligand via the pyridine-type nitrogen of the benzimidazole moiety and the carbamate group. Three-step ionization with pKa values of 3.38, 4.06 and 10.07 were reported for FBZ. The coordination of FBZ to the metal ions led to an increase in the antibacterial activity against the tested Staphylococcus aureus and Escherichia coli bacteria.

Design, optimization, and biological evaluation of novel keto-benzimidazoles as potent and selective inhibitors of phosphodiesterase 10A (PDE10A).

Science.gov (United States)

Hu, Essa; Kunz, Roxanne K; Chen, Ning; Rumfelt, Shannon; Siegmund, Aaron; Andrews, Kristin; Chmait, Samer; Zhao, Sharon; Davis, Carl; Chen, Hang; Lester-Zeiner, Dianna; Ma, Ji; Biorn, Christopher; Shi, Jianxia; Porter, Amy; Treanor, James; Allen, Jennifer R

2013-11-14

Our development of PDE10A inhibitors began with an HTS screening hit (1) that exhibited both high p-glycoprotein (P-gp) efflux ratios in rat and human and poor metabolic stability. On the basis of cocrystal structure of 1 in human PDE10A enzyme, we designed a novel keto-benzimidazole 26 with comparable PDE10A potency devoid of efflux liabilities. On target in vivo coverage of PDE10A in rat brain was assessed using our previously reported LC-MS/MS receptor occupancy (RO) technology. Compound 26 achieved 55% RO of PDE10A at 30 mg/kg po and covered PDE10A receptors in rat brain in a dose-dependent manner. Cocrystal structure of 26 in PDE10A confirmed the binding mode of the novel scaffold. Further optimization resulted in the identification of keto-benzimidazole 34, which showed an increased in vivo efficacy of 57% RO in rats at 10 mg/kg po and an improved in vivo rat clearance and oral bioavailability.

DTPA: Bis benzimidazole as multi model imaging agent

International Nuclear Information System (INIS)

Srivastava, Vikas; Tiwari, A.K.; Sharma, H.; Sharma, R.; Mishra, A.K.

2010-01-01

Full text: The DTPA bis benzimidazole analogue has been tested for radiopharmaceutical efficacy. The radiolabelling was found more then 98% after 8 hrs and blood kinetics was fast. The compound was also tested for optical imaging agent. The Eu 3+ ion has an absorption band in the visible spectrum (578-582 nm) whose wavelength is very sensitive to even small changes in the coordination environment. Although the intensity of this 7F0 → 5D0 transition is low, the bands are relatively narrow, which allows distinguishing different coordination states of the metal. For Eu 3+ complexes which have two differently hydrated forms in aqueous solution, one observes two absorption bands belonging to the two species. High-resolution UV-visible spectra were recorded in aqueous solutions which show a temperature invariant absorption with two distinct, temperature-dependent absorption bands. The intensity ratio of these two bands changes with temperature: the band at shorter wavelengths is decreasing very slightly, while that at longer wavelengths is increasing with the temperature. The ratio of the integrals of the two bands is related to the equilibrium constant, and its temperature dependence yields the reaction enthalpy and entropy

Component and system tests of the SLD Cerenkov Ring Imaging Detector

International Nuclear Information System (INIS)

Antilogus, P.; Bird, F.; Aston, D.; Dasu, S.; Dunwoodie, W.; Hallewell, G.; Kawahara, H.; Kwon, Y.; Leith, D.; Nagamine, T.; Pavel, T.; Muller, D.; Williams, S.; Bienz, T.; Dolinsky, S.; Solodov, E.; Coyle, P.; Cavalli-Sforza, M.; Coyne, D.; Gagnon, P.; Liu, X.; Williams, D.A.

1990-01-01

The components of the SLD barrel Cerenkov Ring Imaging Detector (CRID) are now built and are being installed. This paper reports on tests of these components, including tests of the fiber optic calibration system, detailed studies of electron drift paths on production drift boxes and detectors, tests of the dynamic gating system and its effect on drift path distortions due to space-charge, and a measurement of the electron lifetime in a production drift box. In addition, the authors report on the UV transmission of recirculated liquid freon and on the effects of CRID construction materials on electron lifetime

Component and system tests of the SLD Cerenkov Ring Imaging Detector

International Nuclear Information System (INIS)

Antilogus, P.; Aston, D.; Bienz, T.; Bird, F.; Dasu, S.; Dolinsky, S.; Dunwoodie, W.; Hallewell, G.; Kawahara, H.; Kwon, Y.; Leith, D.; Muller, D.; Nagamine, T.; Pavel, T.; Ratcliff, B.; Rensing, P.; Schultz, D.; Shapiro, S.; Simopoulos, C.; Solodov, E.; Toge, N.; Va'vra, J.; Williams, S.; Cavalli-Sforza, M.; Coyle, P.; Coyne, D.; Gagnon, P.; Liu, X.; Williams, D.A.; Whitaker, J.S.; Wilson, R.J.; Bean, A.; Caldwell, D.; Duboscq, J.; Huber, J.; Lu, A.; Mathys, L.; McHugh, S.; Witherell, M.; Yellin, S.; D'Oliveira, A.; Johnson, R.A.; Martinez, J.L.; Meadows, B.; Nussbaum, M.; Santha, A.K.S.; Shoup, A.; Stockdale, I.; Baird, K.; Jacques, P.; Kalelkar, M.; Plano, R.; Stamer, P.; Word, G.; Abe, K.; Hasegawa, K.; Suekane, F.; Yuta, H.

1991-02-01

The components of the SLD barrel Cerenkov Ring Imaging Detector (CRID) are now built and are being installed. We report on tests of these, including tests of the fiber optic calibration system, detailed studies of electron drift paths on production drift boxes and detectors, tests of the dynamic gating system and its effect on drift path distortions due to space-charge, and a measurement of the electron lifetime in a production drift box. In addition, we report on the UV transmission of recirculated liquid C 6 F 14 and on the effects of CRID construction materials on electron lifetime. 9 refs., 11 figs

Component and system tests of the SLD Cerenkov Ring Imaging Detector

International Nuclear Information System (INIS)