Author | Lopes, Marcela Silva | |
Author | Pietra, Renata Celi Carvalho de Souza | |
Author | Borgati, Tatiane Freitas | |
Author | Romeiro, Carla Fontana Dolabella | |
Author | Sales Junior, Policarpo Ademar | |
Author | Romanha, Alvaro Jose | |
Author | Alves, Ricardo Jose | |
Author | Fagundes, Elaine Maria de Souza | |
Author | Fernandes, Ana Paula Salles Moura | |
Author | Oliveira, Renata Barbosa de | |
Access date | 2015-08-26T18:49:03Z | |
Available date | 2015-08-26T18:49:03Z | |
Document date | 2011 | |
Citation | LOPES, Marcela Silva et al. Synthesis and evaluation of the anti parasitic activity of aromatic nitro compounds. Eur J Med Chem., vol. 46, n. 11, p. 5443-5447, 2011. | pt_BR |
ISSN | 0223-5234 | |
URI | https://www.arca.fiocruz.br/handle/icict/11654 | |
Language | eng | pt_BR |
Publisher | Editions Scientifiques Elsevier | pt_BR |
Rights | restricted access | pt_BR |
Title | Synthesis and evaluation of the anti parasitic activity of aromatic nitro compounds. | pt_BR |
Type | Article | |
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 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. | pt_BR |
Affilliation | Universidade Federal de Minas Gerais. Faculdade de Farmácia. Departamento de Produtos Farmacêuticos. Belo Horizonte, MG, Brazil | pt_BR |
Affilliation | Universidade Federal de Minas. Faculdade de Farmácia. Departamento de Análises Clínicas e Toxicológicas. Belo Horizonte, MG, Brazil | pt_BR |
Affilliation | Universidade Federal de Minas Gerais. Faculdade de Farmácia. Departamento de Produtos Farmacêuticos. Belo Horizonte, MG, Brazil | pt_BR |
Affilliation | Universidade Federal de Minas. Instituto de Ciências Biológicas. Departamento de Fisiologia e Biofísica. Belo Horizonte, MG, Brazil | pt_BR |
Affilliation | Fundação Oswaldo Cruz. Centro de Pesquisas René Rachou. Belo Horizonte, MG, Brazil | pt_BR |
Affilliation | Fundação Oswaldo Cruz. Centro de Pesquisas René Rachou. Belo Horizonte, MG, Brazil | pt_BR |
Affilliation | Universidade Federal de Minas Gerais. Faculdade de Farmácia. Departamento de Produtos Farmacêuticos. Belo Horizonte, MG, Brazil | pt_BR |
Affilliation | Universidade Federal de Minas. Instituto de Ciências Biológicas. Departamento de Fisiologia e Biofísica. Belo Horizonte, MG, Brazil | pt_BR |
Affilliation | Universidade Federal de Minas. Faculdade de Farmácia. Departamento de Análises Clínicas e Toxicológicas. Belo Horizonte, MG, Brazil | pt_BR |
Affilliation | Universidade Federal de Minas Gerais. Faculdade de Farmácia. Departamento de Produtos Farmacêuticos. Belo Horizonte, MG, Brazil | pt_BR |
Subject | Nitro compounds | pt_BR |
Subject | Antileishmanial activity | pt_BR |
Subject | L. amazonensis | pt_BR |
Subject | Trypanocidal | pt_BR |