Cruzain inhibition by hydroxymethylnitrofurazone and nitrofurazone: investigation of a new target in Trypanosoma cruzi
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Data
2010-02-01
Autores
Trossini, Gustavo H. G.
Malvezzi, Alberto
T-do Amaral, Antonia
Rangel-Yagui, Carlota Oliveira
Izidoro, Mario A.
Cezari, Maria Helena S.
Juliano, Luiz
Chin, Chung Man [UNESP]
Menezes, Carla M. S.
Ferreira, Elizabeth Igne
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Editor
Taylor & Francis Ltd
Resumo
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.
Descrição
Palavras-chave
Chagas', disease, cruzain inhibitory activity, molecular modeling, nitrofurazone derivative, Trypanosoma cruzi
Como citar
Journal of Enzyme Inhibition and Medicinal Chemistry. Abingdon: Taylor & Francis Ltd, v. 25, n. 1, p. 62-67, 2010.