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- Cruzain inhibition by hydroxymethylnitrofurazone and nitrofurazone: investigation of a new target in Trypanosoma cruzi
- Universidade de São Paulo (USP)
- Universidade Federal de São Paulo (UNIFESP)
- Universidade Estadual Paulista (UNESP)
- Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)
- Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)
- Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)
- PRP-USP Procontes
- FAPESP: 01/01192-3
- FAPESP: 04/06097-7
- FAPESP: 02/09518-8
- 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.
- Journal of Enzyme Inhibition and Medicinal Chemistry. Abingdon: Taylor & Francis Ltd, v. 25, n. 1, p. 62-67, 2010.
- Taylor & Francis Ltd
- cruzain inhibitory activity
- molecular modeling
- nitrofurazone derivative
- Trypanosoma cruzi
- Acesso restrito
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