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

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dc.contributor.author Trossini, Gustavo H. G.
dc.contributor.author Malvezzi, Alberto
dc.contributor.author T-do Amaral, Antonia
dc.contributor.author Rangel-Yagui, Carlota Oliveira
dc.contributor.author Izidoro, Mario A. [UNIFESP]
dc.contributor.author Cezari, Maria Helena S. [UNIFESP]
dc.contributor.author Juliano, Luiz [UNIFESP]
dc.contributor.author Chin, Chung Man
dc.contributor.author Menezes, Carla M. S.
dc.contributor.author Ferreira, Elizabeth Igne
dc.date.accessioned 2016-01-24T13:59:18Z
dc.date.available 2016-01-24T13:59:18Z
dc.date.issued 2010-02-01
dc.identifier http://dx.doi.org/10.3109/14756360902941058
dc.identifier.citation Journal of Enzyme Inhibition and Medicinal Chemistry. Abingdon: Taylor & Francis Ltd, v. 25, n. 1, p. 62-67, 2010.
dc.identifier.issn 1475-6366
dc.identifier.uri http://repositorio.unifesp.br/handle/11600/32259
dc.description.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. en
dc.description.sponsorship Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)
dc.description.sponsorship Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)
dc.description.sponsorship PROBRAL
dc.description.sponsorship Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)
dc.description.sponsorship PRP-USP Procontes
dc.format.extent 62-67
dc.language.iso eng
dc.publisher Taylor & Francis Ltd
dc.relation.ispartof Journal of Enzyme Inhibition and Medicinal Chemistry
dc.rights Acesso restrito
dc.subject Chagas' en
dc.subject disease en
dc.subject cruzain inhibitory activity en
dc.subject molecular modeling en
dc.subject nitrofurazone derivative en
dc.subject Trypanosoma cruzi en
dc.title Cruzain inhibition by hydroxymethylnitrofurazone and nitrofurazone: investigation of a new target in Trypanosoma cruzi en
dc.type Artigo
dc.rights.license http://journalauthors.tandf.co.uk/permissions/reusingOwnWork.asp
dc.contributor.institution Universidade de São Paulo (USP)
dc.contributor.institution Universidade Federal de São Paulo (UNIFESP)
dc.contributor.institution Univ Estadual Paulista
dc.description.affiliation Univ São Paulo, Fac Ciencias Farmaceut, Dept Farm, BR-05508900 São Paulo, Brazil
dc.description.affiliation Univ São Paulo, Dept Quim Fundamental, Inst Quim, BR-05508900 São Paulo, Brazil
dc.description.affiliation Universidade Federal de São Paulo, Escola Paulista Med, INFAR, Dept Biofis, São Paulo, Brazil
dc.description.affiliation Univ Estadual Paulista, Fac Ciencias Farmaceut, São Paulo, Brazil
dc.description.affiliationUnifesp Universidade Federal de São Paulo, Escola Paulista Med, INFAR, Dept Biofis, São Paulo, Brazil
dc.description.sponsorshipID FAPESP: 01/01192-3
dc.description.sponsorshipID FAPESP: 04/06097-7
dc.description.sponsorshipID FAPESP: 02/09518-8
dc.identifier.doi 10.3109/14756360902941058
dc.description.source Web of Science
dc.identifier.wos WOS:000275000900008



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