title: Synthesis and evaluation of the anti parasitic activity of aromatic nitro compounds.
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.
authors.affiliation: Departamento de Produtos Farmacêuticos, Faculdade de Farmácia, Universidade Federal de Minas Gerais, Avenida Antônio Carlos 6627, Belo Horizonte, MG 31.270-901, Brazil.
authors.forename: Marcela S
authors.initials: MS
authors.lastname: Lopes
authors.forename: Renata C C
authors.initials: RC
authors.lastname: de Souza Pietra
authors.forename: Tatiane F
authors.initials: TF
authors.lastname: Borgati
authors.forename: Carla F D
authors.initials: CF
authors.lastname: Romeiro
authors.forename: Policarpo A S
authors.initials: PA
authors.lastname: Júnior
authors.forename: Alvaro J
authors.initials: AJ
authors.lastname: Romanha
authors.forename: Ricardo J
authors.initials: RJ
authors.lastname: Alves
authors.forename: Elaine M
authors.initials: EM
authors.lastname: Souza-Fagundes
authors.forename: Ana Paula S M
authors.initials: AP
authors.lastname: Fernandes
authors.forename: Renata B
authors.initials: RB
authors.lastname: de Oliveira
mesh_terms: D000977:Antiparasitic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity; D002470:Cell Survival / Q000187:drug effects; D060326:Chemistry Techniques, Synthetic; D006801:Humans; D020128:Inhibitory Concentration 50; D007891:Leishmania / Q000187:drug effects; D008214:Lymphocytes / Q000166:cytology / Q000187:drug effects; D009574:Nitro Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity; D014349:Trypanosoma cruzi / Q000187:drug effects
chemical_list: D000977:Antiparasitic Agents; D009574:Nitro Compounds