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Molecules 2015, 20(1), 43-51; doi:10.3390/molecules20010043

Synthesis and Anti-Trypanosoma cruzi Activity of Diaryldiazepines

1
Departamento de Química, ICEB, Universidade Federal de Ouro Preto, Campus Morro do Cruzeiro, CEP, Ouro Preto, MG 35400-000, Brazil
2
Laboratório de Imunopatologia, Núcleo de Pesquisas em Ciências Biológicas, ICEB II, Morro do Cruzeiro, Universidade Federal de Ouro Preto, Ouro Preto 35400-000, Brazil
*
Author to whom correspondence should be addressed.
Academic Editor: Derek J. McPhee
Received: 14 October 2014 / Accepted: 18 November 2014 / Published: 23 December 2014
(This article belongs to the Section Medicinal Chemistry)
View Full-Text   |   Download PDF [711 KB, uploaded 23 December 2014]   |  

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. View Full-Text
Keywords: diaryldiazepines; Trypanosoma cruzi; Chagas disease; epimastigote diaryldiazepines; Trypanosoma cruzi; Chagas disease; epimastigote
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

Menezes, J.C.L.; Vaz, L.B.A.; de Abreu Vieira, P.M.; da Silva Fonseca, K.; Carneiro, C.M.; Taylor, J.G. Synthesis and Anti-Trypanosoma cruzi Activity of Diaryldiazepines. Molecules 2015, 20, 43-51.

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