SÃntese e avaliaÃÃo da atividade biolÃgica de novos derivados arilazo-imidazolidÃnicos e arilideno-tiazolidÃnicos frente a vermes adultos de Schistosoma mansoni (Cepa BH)

AUTOR(ES)
DATA DE PUBLICAÇÃO

2004

RESUMO

Several biological activities, includding anti-parasitic, are attributed to imidazolidinic and thiazolodinic nucleous due to their chemical reactivite and, consequently afinity; wich directed us to find new antischistossomal agents. We prepared new 5-arylazo-3-benzyl-4-thioxo-imidazolidin-2-one 8a-d and 5-arylidene-3-(4-bromo-benzyl)-thiazolidine-2,4-dione 15a-b derivates. The substituition on the three-position of the heterocyclic ring, in alkaline medium, was done using substituited benzyl chloride or 4-bromo-benzyl bromide in imidazolidine and thiazolidinic rings, respectivaly. A thionation was done at four-position in the derivate 3-benzyl-imidazolidine-2,4-dione. Then, was done the five-position substituition by Michael addition with 3-(4-bromobenzyl)- thiazolidine-2,4-dione and substituited ethyl 3-aryl-2-cyane-acrilates. The 3-benzyl-4-thioxo-imidazolidin-2-one did a diazo coppuling with substituited anilines. The chemical structures of the new compounds was proved by infrarred spectra and hydrogen nuclear magnetic ressonance. The arylazo-imidazolidinic derivates tested (8a-c) showed biological activity against Schistosoma mansoni (Cepa BH) adult worms, being distinguished the derivative 5-(4-fluorine-arylazo)-3-benzyl-4-thioxoimidazolidin-2-one ( 8b, 10 - 80 mg/mL), that exibhited 100% mortality in 24 hours after the treatment, wihch was the best result

ASSUNTO(S)

quimica dos produtos naturais atividade biolÃgica - sÃntese e avaliaÃÃo arilazo-imidazolidÃnicos arilideno-tiazolidÃnicos schistosoma mansoni - vermes adultos

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