Cruzain inhibition by hydroxymethylnitrofurazone and nitrofurazone: investigation of a new target in Trypanosoma cruzi

Cruzain inhibition by hydroxymethylnitrofurazone and nitrofurazone: investigation of a new target in Trypanosoma cruzi

Author Trossini, Gustavo H. G. Google Scholar
Malvezzi, Alberto Google Scholar
T-do Amaral, Antonia Google Scholar
Rangel-Yagui, Carlota Oliveira Google Scholar
Izidoro, Mario A. Autor UNIFESP Google Scholar
Cezari, Maria Helena S. Autor UNIFESP Google Scholar
Juliano, Luiz Autor UNIFESP Google Scholar
Chin, Chung Man Google Scholar
Menezes, Carla M. S. Google Scholar
Ferreira, Elizabeth Igne Google Scholar
Institution Universidade de São Paulo (USP)
Universidade Federal de São Paulo (UNIFESP)
Univ Estadual Paulista
Abstract Nitrofurazone (NF) and its derivative, hydroxymethylnitrofurazone (NFOH), have presented antichagasic activity. NFOH has higher activity and lower mutagenicity. the aim of this work was to assess whether NF and its derivative NFOH would also be inhibitors of cruzain, besides their trypanothione reductase inhibitory activity. in vitro cruzain inhibition tests were performed for both compounds, and the 50% inhibitory concentration (IC(50)) for NF and NFOH presented values of 22.83 +/- 1.2 mu M and 10.55 +/- 0.81 mu M, respectively. AM1 semi-empirical molecular modeling studies were performed to understand the activity of the compounds, corroborating the observed cruzain inhibitory activity.
Keywords Chagas'
disease
cruzain inhibitory activity
molecular modeling
nitrofurazone derivative
Trypanosoma cruzi
Language English
Sponsor Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)
Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)
PROBRAL
Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)
PRP-USP Procontes
Grant number FAPESP: 01/01192-3
FAPESP: 04/06097-7
FAPESP: 02/09518-8
Date 2010-02-01
Published in Journal of Enzyme Inhibition and Medicinal Chemistry. Abingdon: Taylor & Francis Ltd, v. 25, n. 1, p. 62-67, 2010.
ISSN 1475-6366 (Sherpa/Romeo, impact factor)
Publisher Taylor & Francis Ltd
Extent 62-67
Origin http://dx.doi.org/10.3109/14756360902941058
Access rights Closed access
Type Article
Web of Science ID WOS:000275000900008
URI http://repositorio.unifesp.br/handle/11600/32259

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