Autor |
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 ![]() Menezes, Carla M. S. ![]() Ferreira, Elizabeth Igne ![]() |
Instituição | Universidade de São Paulo (USP) Universidade Federal de São Paulo (UNIFESP) Univ Estadual Paulista |
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. |
Assunto |
Chagas'
disease cruzain inhibitory activity molecular modeling nitrofurazone derivative Trypanosoma cruzi |
Idioma | Inglês |
Financiador |
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 |
Número do financiamento |
|
Data | 2010-02-01 |
Publicado em | Journal of Enzyme Inhibition and Medicinal Chemistry. Abingdon: Taylor & Francis Ltd, v. 25, n. 1, p. 62-67, 2010. |
ISSN | 1475-6366 (Sherpa/Romeo, fator de impacto) |
Editor | Taylor & Francis Ltd |
Extensão | 62-67 |
Fonte |
|
Direito de acesso | Acesso restrito |
Tipo | Artigo |
Web of Science | WOS:000275000900008 |
URI | http://repositorio.unifesp.br/handle/11600/32259 |
Arquivos | Tamanho | Formato | Visualização |
---|---|---|---|
Não existem arquivos associados a este item. |