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Bioorg Med Chem Lett ; 24(7): 1707-10, 2014 Apr 01.
Artigo em Inglês | MEDLINE | ID: mdl-24630563

RESUMO

Trypanosoma brucei and Trypanosoma cruzi are the etiologic agents of sleeping sickness and Chagas disease, respectively, two of the 17 preventable tropical infectious diseases (NTD) which have been neglected by governments and organizations working in the health sector, as well as pharmaceutical industries. High toxicity and resistance are problems of the conventional drugs employed against trypanosomiasis, hence the need for the development of new drugs with trypanocidal activity. In this work we have evaluated the trypanocidal activity of a series of N1,N2-dibenzylethane-1,2-diamine hydrochlorides (benzyl diamines) and N1-benzyl,N2-methyferrocenylethane-1,2-diamine hydrochlorides (ferrocenyl diamines) against T. brucei and T. cruzi parasite strains. We show that incorporation of the ferrocenyl group into the benzyl diamines increases the trypanocidal activity. The molecules exhibit potential trypanocidal activity in vitro against all parasite strains. Cytotoxicity assay was also carried out to evaluate the toxicity in HepG2 cells.


Assuntos
Compostos de Benzil/farmacologia , Diaminas/farmacologia , Compostos Ferrosos/farmacologia , Tripanossomicidas/farmacologia , Trypanosoma brucei brucei/efeitos dos fármacos , Trypanosoma cruzi/efeitos dos fármacos , Compostos de Benzil/síntese química , Compostos de Benzil/química , Sobrevivência Celular/efeitos dos fármacos , Diaminas/síntese química , Diaminas/química , Relação Dose-Resposta a Droga , Compostos Ferrosos/síntese química , Compostos Ferrosos/química , Células Hep G2 , Humanos , Metalocenos , Estrutura Molecular , Testes de Sensibilidade Parasitária , Relação Estrutura-Atividade , Tripanossomicidas/síntese química , Tripanossomicidas/química
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