Synthesis and evaluation of the anti parasitic activity of aromatic nitro compounds |
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| Authors: | Lopes Marcela S de Souza Pietra Renata C C Borgati Tatiane F Romeiro Carla F D Júnior Policarpo A S Romanha Alvaro J Alves Ricardo J Souza-Fagundes Elaine M Fernandes Ana Paula S M de Oliveira Renata B |
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| Affiliation: | aDepartamento de Produtos Farmacêuticos, Faculdade de Farmácia, Universidade Federal de Minas Gerais (UFMG), Avenida Antônio Carlos 6627, Belo Horizonte, MG 31.270-901, Brazil;bDepartamento de Análises Clínicas e Toxicológicas, Faculdade de Farmácia, Universidade Federal de Minas, Gerais (UFMG), Brazil;cDepartamento de Fisiologia e Biofísica, Instituto de Ciências Biológicas, Universidade Federal de Minas, Gerais (UFMG), Brazil;dCentro de Pesquisas René Rachou-Fiocruz, Belo Horizonte, MG, Brazil |
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| Abstract: | 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. |
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| Keywords: | Nitro compounds Antileishmanial activity L. amazonensis Trypanocidal T. cruzi |
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