Trypanosoma cruzi: effect and mode of action of nitroimidazole and nitrofuran derivatives

Maya, JD; Bollo, S; Nunez-Vergara, LJ; Squella, JA; Repetto Y; Morello A.; Perie, J; Chauviere, G

Abstract

With the aim of determining the actual target(s) of nitro-group bearing compounds considered as possible leads for the development of drugs against Chagas' disease, we studied in parallel nitrofurans and nitroimidazoles. We investigated nine representative compounds for the following properties: efficacy on different Trypanosoma cruzi strains, redox cyclers, inhibition of respiration, production of corresponding nitroso derivatives and intracellular thiol scavengers. Our results indicate that nifurtimox and related compounds act as redox cyclers, whereas the most active in the series, the 5-nitroimidazole megazol essentially acts as thiol scavenger particularly for trypanothione, the cofactor for trypanothione reductase, an essential enzyme in the detoxification process. © 2003 Elsevier Science Inc. All rights reserved.

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Título según WOS: Trypanosoma cruzi: effect and mode of action of nitroimidazole and nitrofuran derivatives
Título según SCOPUS: Trypanosoma cruzi: Effect and mode of action of nitroimidazole and nitrofuran derivatives
Título de la Revista: BIOCHEMICAL PHARMACOLOGY
Volumen: 65
Número: 6
Editorial: PERGAMON-ELSEVIER SCIENCE LTD
Fecha de publicación: 2003
Página de inicio: 999
Página final: 1006
Idioma: English
URL: http://linkinghub.elsevier.com/retrieve/pii/S0006295202016635
DOI:

10.1016/S0006-2952(02)01663-5

Notas: ISI, SCOPUS