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

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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 [UNESP]
dc.contributor.authorMenezes, Carla M. S.
dc.contributor.authorFerreira, Elizabeth Igne
dc.contributor.institutionUniversidade de São Paulo (USP)
dc.contributor.institutionUniversidade Federal de São Paulo (UNIFESP)
dc.contributor.institutionUniversidade Estadual Paulista (Unesp)
dc.date.accessioned2014-05-20T13:24:56Z
dc.date.available2014-05-20T13:24:56Z
dc.date.issued2010-02-01
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.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.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.description.sponsorshipIdFAPESP: 01/01192-3
dc.description.sponsorshipIdFAPESP: 04/06097-7
dc.description.sponsorshipIdFAPESP: 02/09518-8
dc.format.extent62-67
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.doi10.3109/14756360902941058
dc.identifier.issn1475-6366
dc.identifier.lattes9734333607975413
dc.identifier.orcid0000-0003-4141-0455
dc.identifier.urihttp://hdl.handle.net/11449/7864
dc.identifier.wosWOS:000275000900008
dc.language.isoeng
dc.publisherTaylor & Francis Ltd
dc.relation.ispartofJournal of Enzyme Inhibition and Medicinal Chemistry
dc.relation.ispartofjcr3.638
dc.relation.ispartofsjr1,040
dc.rights.accessRightsAcesso restrito
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.typeArtigo
dcterms.licensehttp://informahealthcare.com/userimages/ContentEditor/1255620309227/Copyright_And_Permissions.pdf
dcterms.rightsHolderTaylor & Francis Ltd
dspace.entity.typePublication
unesp.author.lattes9734333607975413[8]
unesp.author.orcid0000-0003-4141-0455[8]
unesp.author.orcid0000-0003-3634-2531[1]
unesp.author.orcid0000-0003-4221-9505[4]
unesp.author.orcid0000-0003-2087-033X[10]
unesp.author.orcid0000-0002-5589-2822[7]
unesp.author.orcid0000-0003-2937-5255[3]
unesp.campusUniversidade Estadual Paulista (UNESP), Faculdade de Ciências Farmacêuticas, Araraquarapt
unesp.departmentFármacos e Medicamentos - FCFpt

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Araraquara - FCF - Faculdade de Ciências Farmacêuticas