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Title: Synthesis and anti-Trypanosoma cruzi activity of diaryldiazepines.
Authors: Menezes, Júlio César L.
Vaz, Luana Beatriz Araújo
Vieira, Paula Melo de Abreu
Fonseca, Kátia da Silva
Carneiro, Cláudia Martins
Taylor, Jason Guy
Keywords: Diaryldiazepines
Trypanosoma cruzi
Chagas disease
Issue Date: 2015
Citation: MENEZES, J. C. L. et al. Synthesis and anti-Trypanosoma cruzi activity of diaryldiazepines. Molecules, v. 20, p. 43-51, 2015. Disponível em: <>. Acesso em: 20 abr. 2017.
Abstract: Chagas disease is a so-called “neglected disease” and endemic to Latin America. Nifurtimox and benznidazole are drugs that have considerable efficacy in the treatment of the acute phase of the disease but cause many significant side effects. Furthermore, in the Chronic Phase its efficiency is reduced and their therapeutic effectiveness is dependent on the type of T. cruzi strain. For this reason, the present work aims to drive basic research towards the discovery of new chemical entities to treat Chagas disease. Differently substituted 5,7-diaryl-2,3-dihydro-1,4-diazepines were synthesized by cyclocondensation of substituted flavones with ethylenediamine and tested as anti-Trypanosoma cruzi candidates. Epimastigotes of the Y strain from T. cruzi were used in this study and the number of parasites was determined in a Neubauer chamber. The most potent diaryldiazepine that reduced epimastigote proliferation exhibited an IC50 value of 0.25 μM, which is significantly more active than benznidazole.
ISSN: 1420-3049
Appears in Collections:DEQUI - Artigos publicados em periódicos

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