In vitro trypanocidal activity of nitroimidazole derivatives

Chagas' disease, caused by the protozoan parasite Trypanosoma cruzi, affects 9-12 million of people in Latin America and it is an important cause of heart disease. Although transmission has been reduced, an effective therapy for the infected population is lacking. New isomers nitroimidazole der...

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Autores principales: Ramos Ligonio, Ángel, López Monteon, Aracely, Carrera Huerta, Francisco, García Gálvez, Ana M., Márquez López , Elizabeth, Sánchez Pavón, Esmeralda
Formato: Articulo
Lenguaje:Inglés
Publicado: 2012
Materias:
Acceso en línea:http://sedici.unlp.edu.ar/handle/10915/8429
http://www.latamjpharm.org/resumenes/31/1/LAJOP_31_1_1_9.pdf
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id I19-R120-10915-8429
record_format dspace
institution Universidad Nacional de La Plata
institution_str I-19
repository_str R-120
collection SEDICI (UNLP)
language Inglés
topic Farmacia
Trypanosoma cruzi
Nitroimidazoles
Enfermedad de Chagas
spellingShingle Farmacia
Trypanosoma cruzi
Nitroimidazoles
Enfermedad de Chagas
Ramos Ligonio, Ángel
López Monteon, Aracely
Carrera Huerta, Francisco
García Gálvez, Ana M.
Márquez López , Elizabeth
Sánchez Pavón, Esmeralda
In vitro trypanocidal activity of nitroimidazole derivatives
topic_facet Farmacia
Trypanosoma cruzi
Nitroimidazoles
Enfermedad de Chagas
description Chagas' disease, caused by the protozoan parasite Trypanosoma cruzi, affects 9-12 million of people in Latin America and it is an important cause of heart disease. Although transmission has been reduced, an effective therapy for the infected population is lacking. New isomers nitroimidazole derivatives [4(5)-bromo-1-phenacyl-5(4)-nitroimidazoles] were developed and their antichagasic properties were studied. Five compounds (with different substituents in their aromatic ring) displayed remarkable in vitro activities against T. cruzi. The results demonstrated that 4(5)-bromo-1-(4-methoxiphenacyl)-2-methyl-5(4)- nitroimidazole, 4(5)-bromo-1-(4-chlorophenacyl)-2-methyl-5(4)-nitroimidazole, and 4(5)-bromo-1-(4- cianophenacyl)-2-methyl-5(4)-nitroimidazole have IC50 values of of 3.95, 2.3, and 1.15 μg/mL, respectively, and show acceptable values of cytotoxicity, at concentrations below 5 μg/mL. Our results indicate that mixtures of isomers are a potent inhibitor of T. cruzi growth. The present evidence shows very promising results of new isomers, which emerge as strong candidates for further tests as anti-T. cruzi agents.
format Articulo
Articulo
author Ramos Ligonio, Ángel
López Monteon, Aracely
Carrera Huerta, Francisco
García Gálvez, Ana M.
Márquez López , Elizabeth
Sánchez Pavón, Esmeralda
author_facet Ramos Ligonio, Ángel
López Monteon, Aracely
Carrera Huerta, Francisco
García Gálvez, Ana M.
Márquez López , Elizabeth
Sánchez Pavón, Esmeralda
author_sort Ramos Ligonio, Ángel
title In vitro trypanocidal activity of nitroimidazole derivatives
title_short In vitro trypanocidal activity of nitroimidazole derivatives
title_full In vitro trypanocidal activity of nitroimidazole derivatives
title_fullStr In vitro trypanocidal activity of nitroimidazole derivatives
title_full_unstemmed In vitro trypanocidal activity of nitroimidazole derivatives
title_sort in vitro trypanocidal activity of nitroimidazole derivatives
publishDate 2012
url http://sedici.unlp.edu.ar/handle/10915/8429
http://www.latamjpharm.org/resumenes/31/1/LAJOP_31_1_1_9.pdf
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