Departamento de Produtos Farmacêuticos, Faculdade de Farmácia, Universidade Federal de Minas Gerais, Avenida Antônio Carlos 6627, Belo Horizonte, MG 31.270-901, Brazil.
Eur J Med Chem. 2011 Nov;46(11):5443-7. doi: 10.1016/j.ejmech.2011.09.002. Epub 2011 Sep 8.
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.
一系列硝基芳香族化合物被合成并评估为潜在的抗利什曼原虫和锥虫药物。五种化合物对体外的美洲利什曼原虫（L.）亚马逊ensis 前鞭毛体表现出显著的抗利什曼原虫活性，IC50 在 23-59 μmol L（-1）范围内，但对锥虫克鲁兹体内的无鞭毛体形式均无活性。还评估了对植物血凝素（PHA）刺激的人外周血单核细胞（PBMC）增殖的体外细胞毒性。发现两种化合物 6 和 7 具有有希望的抗利什曼原虫活性，IC50 值分别为 59.5 和 50.6 μM，而不影响 PBMC 中的淋巴细胞增殖（选择性指数分别为 16.1 和 21.7），表明对人细胞的毒性低。
