Synthesis and anti-Trypanosoma cruzi activity of diaryldiazepines.
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Data
2015
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Resumo
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.
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Diaryldiazepines, Trypanosoma cruzi, Chagas disease, Epimastigote
Citação
MENEZES, J. C. L. et al. Synthesis and anti-Trypanosoma cruzi activity of diaryldiazepines. Molecules, v. 20, p. 43-51, 2015. Disponível em: <http://www.mdpi.com/1420-3049/20/1/43>. Acesso em: 20 abr. 2017.