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

被引：20
|
作者：
Lopes, Marcela S. [1 ]
de Souza Pietra, Renata C. C. [2 ]
Borgati, Tatiane F. [1 ]
Romeiro, Carla F. D. [3 ]
Junior, Policarpo A. S. [4 ]
Romanha, Alvaro J. [4 ]
Alves, Ricardo J. [1 ]
Souza-Fagundes, Elaine M. [3 ]
Fernandes, Ana Paula S. M. [2 ]
de Oliveira, Renata B. [1 ]
机构：
[1] Univ Fed Minas Gerais, Fac Farm, Dept Produtos Farmaceut, BR-31270901 Belo Horizonte, MG, Brazil
[2] Univ Fed Minas Gerais, Fac Farm, Dept Anal Clin Toxicol, BR-31270901 Belo Horizonte, MG, Brazil
[3] Univ Fed Minas Gerais, Dept Fisiol & Biofis, Inst Ciencias Biol, BR-31270901 Belo Horizonte, MG, Brazil
[4] Ctr Pesquisas Rene Rachou Fiocruz, Belo Horizonte, MG, Brazil
来源：
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2011年 / 46卷 / 11期
关键词：
Nitro compounds; Antileishmanial activity; L; amazonensis; Trypanocidal; T; cruzi; SOLID-PHASE SYNTHESIS; TRYPANOSOMA-CRUZI; CHAGAS-DISEASE; IN-VITRO; LEISHMANIASIS; DRUGS;
D O I：
10.1016/j.ejmech.2011.09.002
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
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 IC50 in the range of 23-59 mu mol 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 IC50 values of 59.5 and 50.6 mu M, respectively, without affecting the lymphocyte proliferation in PBMCs (selectivity index of 16.1 and 21.7, respectively), indicating low toxicity to human cells. (C) 2011 Elsevier Masson SAS. All rights reserved.
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页码：5443 / 5447
页数：5
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