Your browser doesn't support javascript.
loading
Mostrar: 20 | 50 | 100
Resultados 1 - 1 de 1
Filtrar
Mais filtros











Base de dados
Intervalo de ano de publicação
1.
Bioorg Med Chem Lett ; 24(24): 5558-5562, 2014 Dec 15.
Artigo em Inglês | MEDLINE | ID: mdl-25466174

RESUMO

Herewith, we report the design and synthesis of a series of N-(2-oxo-2((4-oxo-2-substituted thiazolidin-3yl)amino)ethyl) benzamide derivatives 7(a-j) under microwave irradiation, based on four component pharmacophoric model to get structural prerequisite indispensable for anticonvulsant activity. The synthesized derivatives were investigated in maximal electroshock seizure (MES), subcutaneous pentylenetetrazole (sc-PTZ) induced seizure and neurotoxicity screening. All the test compounds were administered at a dose of 30, 100 and 300 mg/kg body weight at the time interval of 0.5 h and 4 h. The compounds were also evaluated for behavioral activity and toxicity study. The compound 7 h was found to be most active in MES model. The anticonvulsant screening data shows that 65% of the compounds were found active against MES model when compared to 35% sc-PTZ model. The computational parameter such as docking study, logP determination and ADME prediction were performed to exploit the results.


Assuntos
Anticonvulsivantes/síntese química , Benzamidas/química , Micro-Ondas , Animais , Anticonvulsivantes/farmacologia , Anticonvulsivantes/uso terapêutico , Benzamidas/farmacocinética , Benzamidas/uso terapêutico , Sítios de Ligação , Modelos Animais de Doenças , Meia-Vida , Fígado/patologia , Camundongos , Simulação de Acoplamento Molecular , Atividade Motora/efeitos dos fármacos , Estrutura Terciária de Proteína , Convulsões/tratamento farmacológico , Canais de Sódio/química , Canais de Sódio/metabolismo , Tiazolidinas/química
SELEÇÃO DE REFERÊNCIAS
DETALHE DA PESQUISA