Sample records for triazoles
from WorldWideScience.org

Sample records 1 - 4 shown.



1

Heterociclos 1,2,3-triazólicos: histórico, métodos de preparação, aplicações e atividades farmacológicas/ 1,2,3-triazolic heterocycles: history, preparations, applications and pharmacological activities

Melo, Júlio O. F.; Donnici, Claudio Luis; Augusti, Rodinei; Ferreira, Vitor F.; Souza, Maria Cecília B. V. de; Ferreira, Maria Lourdes G.; Cunha, Anna C.
2006-06-01

Resumo em inglês The 1,2,3-triazole, known since the end of 19th century, is a very widely used heterocyclic system present in many synthetic substances and commercial pharmaceutical compounds. In fact, 1,2,3-triazoles show several applications in many areas especially as medicines against many diseases like cancer, AIDS, Parkinson and Alzheimer. Nowadays there is a large variety of known methods to obtain these heterocyclic compounds comprising mainly three synthetic routes. Nevertheless (mais) , there is no article that gives an objective overview of the synthetic methods for obtaining these kinds of azoheterocycles. This paper presents a brief history of this class of compounds, and a synthetic discussion concerning the main synthetic methods for its preparation, such as cyclization through hydrazones, concerted cycloadditon [2+3] and pseudopericyclic cyclization - and some others of restricted application, but also important. Finally, this paper also provides a brief overview on pharmacological applications of some 1,2,3-triazoles.

Scientific Electronic Library Online (Portuguese)

2

Fungitoxicidade de grupos químicos sobre Myrothecium roridum in vitro e sobre a mancha-de-mirotécio em algodoeiro/ Fungitoxicity of chemical groups on Myrothecium roridum in vitro and on myrothecium leaf spot on cotton plants

Silva, Juliano César da; Meyer, Maurício Conrado; Coutinho, Wirton Macedo; Suassuna, Nelson Dias
2006-05-01

Resumo em português O objetivo deste trabalho foi avaliar a fungitoxicidade de produtos pertencentes aos grupos dos benzimidazóis, triazóis, estrobilurinas, isoftalonitrilas e ditiocarbamatos sobre a germinação conidial e o crescimento micelial in vitro de isolados de Myrothecium roridum e, in vivo, sobre a severidade da mancha-de-mirotécio em plantas de algodoeiro. Nos testes in vitro os fungicidas foram solubilizados em meio BDA, utilizando-se as concentrações de 0,1, 1, 10 e 100 mg (mais) L-1 de ingrediente ativo. A fungitoxidade dos produtos foi avaliada por meio da ED50 (dose necessária para inibir 50% da germinação conidial ou crescimento micelial). Em casa de vegetação, estimou-se a severidade da mancha-de-mirotécio pela porcentagem de área foliar lesionada nas plantas de algodoeiro tratadas antes (preventivo) e depois (curativo) da inoculação do patógeno. Os fungicidas tiofanato metílico, carbendazim, metconazol, tiofanato metílico + clorotalonil, piraclostrobina + epoxiconazol, piraclostrobina + metiram, triflostrobina + propiconazol e tebuconazol inibiram com alta eficácia (ED50 Resumo em inglês The objective of this work was to evaluate the toxicity of benzimidazoles, triazoles, strobilurins, isoftalonitrils and ditiocarbamats on Myrothecium roridum conidial germination and micelial growth in vitro, and the myrothecium leaf spot severity on cotton plants. On in vitro tests, fungicides were solubilized in PDA media at the following concentrations: 0.1, 1, 10 and 100 mg L-1. The toxicity of the products were evaluated by the ED50 rate (required for inhibiting 50% (mais) of the conidial germination or mycelial growth). In greenhouse tests, the severity of myrothecium leaf spot was quantified by measuring the leaf area affected by the pathogen in cotton plants sprayed before (preventive) and after (curative) the pathogen inoculation. The fungicides thiophanate methyl, carbendazim, metconazole, thiophanate methyl + chlorothalonil, pyraclostrobin + epoxyconazole, pyraclostrobin + metiran, trifloxystrobin + propiconazole, and tebuconazole were highly efficient (ED50

Scientific Electronic Library Online (Portuguese)

3

Criptococose: estudo clínico-epidemiológico, laboratorial e das variedades do fungo em 96 pacientes/ Cryptococosis: clinical epidemiologycal laboratorial study and fungi varieties in 96 patients

Moreira, Tomaz de Aquino; Ferreira, Marcelo Simão; Ribas, Rosineide Marques; Borges, Aércio Sebastião
2006-06-01

Resumo em português Estudo prospectivo foi realizado no Hospital de Clínicas da Universidade Federal de Uberlândia, entre março de 1998 e novembro de 2003, em 96 pacientes com diagnóstico clínico e laboratorial de criptococose, sendo 81,3% portadores de Aids. Cepas de Cryptococcus neoformans foram obtidas de diferentes amostras, sendo 77% em líquido cefalorraquidiano. A var neoformans foi isolada em 89 casos e a var gattii em 7. A meningoencefalite criptocócica (56,3% dos casos), foi (mais) a manifestação clínica mais descrita, seguida da fungemia (13,5%). Entre os fatores de risco, a AIDS (81,3%) foi o mais comumente associado à micose. A pesquisa direta do fungo realizada em 121 amostras demonstrou o microrganismo em 98,3%, com cultura (+) em todas. Dos pacientes, 59,4% foram tratados com anfotericina B ou derivados triazólicos, sendo que 72,9% evoluíram para óbito, em particular os portadores de AIDS (62,5%). Atualmente, a criptococose tem sido diagnosticada com muita freqüência em nosso meio e constitui uma das doenças oportunísticas de maior morbidade e mortalidade nos pacientes com AIDS. Resumo em inglês Ninety-six patients with cryptococcosis confirmed by clinical and laboratorial diagnosis were assessed in a prospective study in a University Hospital from March 1998 to November 2003; of these, 81.3% were HIV seropositive patients. Cryptococcus neoformans was isolated from different samples, of which the cerebrospinal fluid 74 (77%) was the most frequent. C. neoformans var neoformans was isolated in 89 cases, where as C. neoformans var gattii was isolated in 7. Cryptococ (mais) cal meningoencephalitis was detected in 56.3% cases. It was the most frequent unique clinical manifestation and the fungus was detected in the bloodstream in 13.5% of the patients. Among the risk factors, AIDS (81.3%) was the most frequently associated with mycosis. Direct examination carried out on 121 samples revealed the microorganism in 98.3% of them, while the culture was positive for all samples. Most of the patients (59.4%) were treated with amphotericin B or with triazoles, however 72.9% of them ended in death, in particular those patients with positive tests for the HIV (62.5%). Nowadays, cryptococcosis has been frequently diagnosed in our region and represents one of the opportunistic diseases with the highest morbidity and mortality rates in patients with AIDS.

Scientific Electronic Library Online (Portuguese)

4

Controvérsias a respeito da sepse fúngica no pré-termo extremo: profilaxia e esquemas terapêuticos/ Controversies about the management of invasive fungal infections in very low birth weight infants

Moreira, Maria E. L.
2005-03-01

Resumo em português OBJETIVO: Rever as mais recentes publicações sobre infecção fúngica no recém-nascido de muito baixo peso ao nascer, com objetivo de fornecer aos profissionais de saúde atualização sobre um crescente problema nas unidades neonatais. A revisão se dirige especificamente às questões relacionadas a incidência, manuseio clínico, tratamento e profilaxia. FONTES DE DADOS: Artigos originais e de revisão, publicados nos últimos 15 anos no MEDLINE e Lilacs, foram ide (mais) ntificados usando como palavras-chave: recém-nascido, prematuro, baixo peso ao nascer, infecção fúngica, sepse, cândida, anfotericina e fluconazol. SÍNTESE DOS DADOS: A incidência de sepse fúngica vem aumentando nas unidades de terapia intensiva neonatal. Embora novas drogas venham se tornando disponíveis (echinocandinas), a anfotericina B continua sendo a droga de escolha para o tratamento inicial. Atualmente, existem quatro classes de drogas disponíveis para o tratamento: os polienos macrolídeos (anfotericina B e formulações lipídicas), os azoles (fluconazol e voriconazol), as pirimidinas fluorinadas (flucitosina) e as echinocandinas (micafungin e caspofungin). Duas drogas vêm sendo descritas na prevenção da doença invasiva: nistatina e fluconazol. Fluconazol é a droga sobre a qual mais se conhece da farmacocinética no período neonatal, e a sua administração profilática em recém-nascidos com menos de 1.000 g por 6 semanas está associada a menor incidência de infecção fúngica. CONCLUSÕES: Um melhor entendimento sobre a incidência da sepse fúngica, diagnóstico, manuseio clínico, tratamento e profilaxia é uma importante arma na morbidade e mortalidade. A identificação de recém-nascidos prematuros de alto risco para o desenvolvimento da doença e a instituição de medidas profiláticas e tratamento precoce podem diminuir a morbimortalidade. Resumo em inglês OBJECTIVE: This review encompasses the most recent publications about fungal infection in very low birth weight infants, keeping health professionals updated about this growing problem observed in neonatal units. SOURCES OF DATA: Original and review articles published over the past 15 years were searched in MEDLINE and Lilacs, using the following keywords: preterm infant, very low birth weight infants, sepsis, fungal infection, antifungal, Candida, amphotericin and flucon (mais) azole. SUMMARY OF THE FINDINGS: Invasive fungal infections affect especially preterm infants. Although new drugs (echinocandins) to treat fungal infection are available, amphotericin is the most widely used drug for the treatment of systemic candidiasis at this stage of life. Currently, there are four types of antifungal agents used in the treatment of fungal infections in neonates: polyene macrolides (amphotericin B deoxycholate and lipid preparations), azoles (triazoles), fluorinated pyrimidines (flucytosine) and echinocandins (caspofungin and micafungin). Two drugs capable of preventing invasive fungal infection are described: nystatin and fluconazole. The pharmacokinetics of fluconazole in the neonatal period is widely known and its prophylactic administration during the first six weeks of life has been associated with less invasive fungal infection in infants weighing less than 1,000 g at birth. CONCLUSIONS: Fungal infections constitute an important problem in the neonatal intensive care unit and a better understanding of the incidence, diagnosis, clinical management, treatment, and prophylaxis is important in order to reduce morbidity and mortality. The identification of high-risk preterm infants and the implementation of prophylactic measures and early treatment may improve the outcome of these patients.

Scientific Electronic Library Online (Portuguese)