Sample records for hydrazones

Sample records 1 - 3 shown.


Síntese e avaliação preliminar da atividade antinociceptiva de novas isoxazolil-aril-hidrazonas/ Synthesis and preliminary evaluation of antinociceptive activity of novel isoxazolyl-aryl-hydrazones

Reis, Sílvio Leandro Gonçalves Bomfim; Almeida, Valderes Moraes de; Almeida, Gleybson Correia de; Boaviagem, Karinna Moura; Mendes, Charles Christophe Du Barriere; Faria, Antônio Rodolfo de; Góes, Alexandre José da Silva; Magalhães, Laudelina Rodrigues; Silva, Teresinha Gonçalves da

Resumo em inglês New 2-isoxazoline aldehydes were synthesized, in good yields, from cycloadduct of the 1,3-dipolar cycloaddition reaction between endocyclic enecarbamate and carboethoxyformonitrile oxide (CEFNO). Condensation of these 2-isoxazoline aldehydes with several phenyl-hydrazines produced new isoxazolyl-aryl-hydrazones, which showed low toxicity and excellent antinociceptive activity, when compared to dipyrone. The antinociceptive activity of isoxazolyl-aryl-hydrazones was performed using the acetic acid-induced mice abdominal constrictions test.

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A química medicinal de N-acilidrazonas: novos compostos-protótipos de fármacos analgésicos, antiinflamatórios e anti-trombóticos/ Medicinal chemistry of N-acylhydrazones: novel lead-compounds of analgesic, antiinflammatory and antithrombotic drugs

Barreiro, Eliezer J.; Fraga, Carlos A. M.; Miranda, Ana L. P.; Rodrigues, Carlos R.

Resumo em inglês In this article are described new bioactive N-acylhydrazone (NAH) derivatives, structurally designed as optimization of aryl hydrazones precursors planned by molecular hybridization of two 5-lipoxigenase inhibitors, e.g. CBS-1108 and BW-755c. The analgesic, antiedematogenic and anti-platelet aggregating profile of several isosteric compounds was investigated by using classic pharmacological assays in vivo and ex-vivo, allowing to identify new potent peripheric analgesic l (mais) ead, a new anti-inflammatory and an antithrombotic agent. During this study was discovered dozen of active NAH compounds clarifying the structure-activity relationship for this series of NAH derivatives, indicating the pharmacophore character of the N-acylhydrazone functionality.

Scientific Electronic Library Online (Portuguese)


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.

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)