2. Academic Validation
  3. Synthesis and evaluation of the anti parasitic activity of aromatic nitro compounds

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

  • Eur J Med Chem. 2011 Nov;46(11):5443-7. doi: 10.1016/j.ejmech.2011.09.002.
Marcela S Lopes 1,  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
Affiliations

Affiliation

  • 1 Departamento de Produtos Farmacêuticos, Faculdade de Farmácia, Universidade Federal de Minas Gerais, Avenida Antônio Carlos 6627, Belo Horizonte, MG 31.270-901, Brazil.
PMID: 21940071 DOI: 10.1016/j.ejmech.2011.09.002
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 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.

Figures