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dc.contributor.authorTrossini, Gustavo H. G.-
dc.contributor.authorMalvezzi, Alberto-
dc.contributor.authorT-do Amaral, Antonia-
dc.contributor.authorRangel-Yagui, Carlota Oliveira-
dc.contributor.authorIzidoro, Mario A.-
dc.contributor.authorCezari, Maria Helena S.-
dc.contributor.authorJuliano, Luiz-
dc.contributor.authorChin, Chung Man-
dc.contributor.authorMenezes, Carla M. S.-
dc.contributor.authorFerreira, Elizabeth Igne-
dc.date.accessioned2014-05-20T13:24:56Z-
dc.date.accessioned2016-10-25T16:45:35Z-
dc.date.available2014-05-20T13:24:56Z-
dc.date.available2016-10-25T16:45:35Z-
dc.date.issued2010-02-01-
dc.identifierhttp://dx.doi.org/10.3109/14756360902941058-
dc.identifier.citationJournal of Enzyme Inhibition and Medicinal Chemistry. Abingdon: Taylor & Francis Ltd, v. 25, n. 1, p. 62-67, 2010.-
dc.identifier.issn1475-6366-
dc.identifier.urihttp://hdl.handle.net/11449/7864-
dc.identifier.urihttp://acervodigital.unesp.br/handle/11449/7864-
dc.description.abstractNitrofurazone (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.sponsorshipFundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)-
dc.description.sponsorshipCoordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)-
dc.description.sponsorshipPROBRAL-
dc.description.sponsorshipConselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)-
dc.description.sponsorshipPRP-USP Procontes-
dc.format.extent62-67-
dc.language.isoeng-
dc.publisherTaylor & Francis Ltd-
dc.sourceWeb of Science-
dc.subjectChagas'en
dc.subjectdiseaseen
dc.subjectcruzain inhibitory activityen
dc.subjectmolecular modelingen
dc.subjectnitrofurazone derivativeen
dc.subjectTrypanosoma cruzien
dc.titleCruzain inhibition by hydroxymethylnitrofurazone and nitrofurazone: investigation of a new target in Trypanosoma cruzien
dc.typeoutro-
dc.contributor.institutionUniversidade de São Paulo (USP)-
dc.contributor.institutionUniversidade Federal de São Paulo (UNIFESP)-
dc.contributor.institutionUniversidade Estadual Paulista (UNESP)-
dc.description.affiliationUniv São Paulo, Fac Ciencias Farmaceut, Dept Farm, BR-05508900 São Paulo, Brazil-
dc.description.affiliationUniv São Paulo, Dept Quim Fundamental, Inst Quim, BR-05508900 São Paulo, Brazil-
dc.description.affiliationUniv Fed São Paulo, Escola Paulista Med, INFAR, Dept Biofis, São Paulo, Brazil-
dc.description.affiliationUniv Estadual Paulista, Fac Ciencias Farmaceut, São Paulo, Brazil-
dc.description.affiliationUnespUniv Estadual Paulista, Fac Ciencias Farmaceut, São Paulo, Brazil-
dc.description.sponsorshipIdFAPESP: 01/01192-3-
dc.description.sponsorshipIdFAPESP: 04/06097-7-
dc.description.sponsorshipIdFAPESP: 02/09518-8-
dc.identifier.doi10.3109/14756360902941058-
dc.identifier.wosWOS:000275000900008-
dc.rights.accessRightsAcesso restrito-
dc.relation.ispartofJournal of Enzyme Inhibition and Medicinal Chemistry-
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