European Journal of Medicinal Chemistry 2011-11-01

Synthesis and evaluation of the anti parasitic activity of aromatic nitro compounds.

Marcela S Lopes, Renata C C de Souza Pietra, Tatiane F Borgati, Carla F D Romeiro, Policarpo A S Júnior, Alvaro J Romanha, Ricardo J Alves, Elaine M Souza-Fagundes, Ana Paula S M Fernandes, Renata B de Oliveira

文献索引：Eur. J. Med. Chem. 46 , 5443-7, (2011)

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摘要

A series of nitroaromatic compounds was synthesized and evaluated as potential antileishmanial and trypanocidal agents. Five compounds exerted significant anti-leishmanial activity in vitro against promastigotes forms of Leishmania (L.) amazonensis, with IC(50) in the range of 23-59 μmol L(-1), but none were active against amastigotes intracellular forms of Trypanosoma cruzi. In vitro cytotoxicity on the proliferation of human peripheral blood mononuclear cells (PBMC) stimulated with phytohemaglutinin (PHA) was also evaluated. Two compounds, 6 and 7, were found to present a promising anti-leishmanial activity with IC(50) values of 59.5 and 50.6 μM, respectively, without affecting the lymphocyte proliferation in PBMCs (selectivity index of 16.1 and 21.7, respectively), indicating low toxicity to human cells.Copyright © 2011 Elsevier Masson SAS. All rights reserved.