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

2011; Elsevier BV; Volume: 46; Issue: 11 Linguagem: Inglês

10.1016/j.ejmech.2011.09.002

1768-3254

Marcela Silva Lopes, Renata Celi Carvalho de Souza Pietra, Tatiane Freitas Borgati, C.F.D. Romeiro, Policarpo Ademar Sales, Álvaro J. Romanha, Ricardo José Alves, Elaine M. Souza–Fagundes, Ana Paula Fernandes, Renata Barbosa de Oliveira,

Synthesis and Biological Evaluation

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 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 IC50 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.