dc.contributorUniversidade de São Paulo (USP)
dc.contributorUniversidade Federal de São Paulo (UNIFESP)
dc.contributorUniversidade Estadual Paulista (Unesp)
dc.date.accessioned2014-05-20T13:24:56Z
dc.date.available2014-05-20T13:24:56Z
dc.date.created2014-05-20T13:24:56Z
dc.date.issued2010-02-01
dc.identifierJournal of Enzyme Inhibition and Medicinal Chemistry. Abingdon: Taylor & Francis Ltd, v. 25, n. 1, p. 62-67, 2010.
dc.identifier1475-6366
dc.identifierhttp://hdl.handle.net/11449/7864
dc.identifier10.3109/14756360902941058
dc.identifierWOS:000275000900008
dc.identifier9734333607975413
dc.identifier0000-0003-4141-0455
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.
dc.languageeng
dc.publisherTaylor & Francis Ltd
dc.relationJournal of Enzyme Inhibition and Medicinal Chemistry
dc.relation3.638
dc.relation1,040
dc.rightsAcesso restrito
dc.sourceWeb of Science
dc.subjectChagas'
dc.subjectdisease
dc.subjectcruzain inhibitory activity
dc.subjectmolecular modeling
dc.subjectnitrofurazone derivative
dc.subjectTrypanosoma cruzi
dc.titleCruzain inhibition by hydroxymethylnitrofurazone and nitrofurazone: investigation of a new target in Trypanosoma cruzi
dc.typeArtículos de revistas


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