Saltar al contenido
Merck

In vitro and in vivo antitrypanosomatid activity of 5-nitroindazoles.

European journal of medicinal chemistry (2008-08-19)
Lucia Boiani, Alejandra Gerpe, Vicente J Arán, Susana Torres de Ortiz, Elva Serna, Ninfa Vera de Bilbao, Luis Sanabria, Gloria Yaluff, Héctor Nakayama, Antonieta Rojas de Arias, Juan Diego Maya, J Antonio Morello, Hugo Cerecetto, Mercedes González
RESUMEN

Previously, we have identified a series of 5-nitroindazoles with good antiprotozoal activities, against Trypanosoma cruzi epimastigotes and Trichomonas vaginalis. Most of them have shown very low unspecific toxicity on macrophage cell lines. In the present work, we assayed these compounds on T. cruzi bloodstream trypomastigotes and Leishmania promastigotes (Leishmania amazonensis, Leishmania braziliensis and Leishmania infantum). Derivatives 1, 2, 7 and 8 displayed remarkable trypanocidal activity (>80% lysis) equivalent to gentian violet. Derivatives 2 and 10, as Pentamidine, caused the complete lysis of promastigotes of Leishmania. An oxidative stress-mediated mechanism of action was confirmed for derivatives 1, 10 and 12 on T. cruzi epimastigotes. Supported by the in vitro activities, derivatives 1 and 2 were submitted to in vivo assays using an acute model of Chagas' disease and a short-term treatment. None of the animals treated with derivatives 1 and 2 died, unlike the untreated control and Benznidazole groups.

MATERIALES
Referencia del producto
Marca
Descripción del producto

Sigma-Aldrich
Crystal Violet, certified by the Biological Stain Commission
Sigma-Aldrich
Crystal Violet, ACS reagent, ≥90.0% anhydrous basis
Sigma-Aldrich
Crystal Violet Solution
Sigma-Aldrich
Crystal Violet Solution
Sigma-Aldrich
Crystal Violet, for microscopy (Bact., Bot., Hist., Vit.), indicator (pH 0.1-2.0)
Supelco
Crystal Violet, VETRANAL®, analytical standard
Sigma-Aldrich
Gentian violet, for microscopy (Bact., Hist.)
Sigma-Aldrich
Gentian Violet, meets USP testing specifications
Sigma-Aldrich
Crystal Violet, indicator for the determination of the redox potential, S. No.: 785