Synthesis and in vitro evaluation of potential antichagasic hydroxymethyinitrofurazone (NFOH-121): A new nitrofurazone prodrug

dc.contributor.authorChung, M. C.
dc.contributor.authorGuido, RVC
dc.contributor.authorMartinelli, T. F.
dc.contributor.authorGoncalves, M. F.
dc.contributor.authorPolli, M. C.
dc.contributor.authorBotelho, KCA
dc.contributor.authorVaranda, Eliana Aparecida [UNESP]
dc.contributor.authorColli, W.
dc.contributor.authorMiranda, MTM
dc.contributor.authorFerreira, E. I.
dc.contributor.institutionUniversidade de São Paulo (USP)
dc.contributor.institutionUniversidade Estadual Paulista (Unesp)
dc.date.accessioned2014-05-20T13:24:38Z
dc.date.available2014-05-20T13:24:38Z
dc.date.issued2003-11-03
dc.description.abstractThe synthesis of mutual prodrugs of nitrofurazone with primaquine, using specific and nonspecific spacer groups, has been previously attempted seeking selective antichagasic agents. The intermediate reaction product, hydroxymethylnitrofurazone (NFOH-121), was isolated and tested in LLC-MK2 culture cells infected with trypomastigotes forms of Trypanosoma cruzi showing higher trypanocidal activity than nitrofurazone and benznidazol in all stages. The mutagenicity tests showed that the prodrug was less toxic than the parent drug. Degradation assays were carried out in pH 1.2 and 7.4. (C) 2003 Elsevier Ltd. All rights reserved.en
dc.description.affiliationUSP, Dept Farm, Fac Ciências Farmaceut, BR-05389970 São Paulo, Brazil
dc.description.affiliationUNESP, Lapdesf Lab Pesquisa & Desenvolvimento Farm, Dept Farmacos & Med, Fac Ciências Farmaceut, BR-14801902 Araraquara, SP, Brazil
dc.description.affiliationUNESP, Dept Ciências Biol, Fac Ciências Farmaceut, BR-14801902 Araraquara, SP, Brazil
dc.description.affiliationUnespUNESP, Lapdesf Lab Pesquisa & Desenvolvimento Farm, Dept Farmacos & Med, Fac Ciências Farmaceut, BR-14801902 Araraquara, SP, Brazil
dc.description.affiliationUnespUNESP, Dept Ciências Biol, Fac Ciências Farmaceut, BR-14801902 Araraquara, SP, Brazil
dc.format.extent4779-4783
dc.identifierhttp://dx.doi.org/10.1016/j.bmc.2003.07.004
dc.identifier.citationBioorganic & Medicinal Chemistry. Oxford: Pergamon-Elsevier B.V., v. 11, n. 22, p. 4779-4783, 2003.
dc.identifier.doi10.1016/j.bmc.2003.07.004
dc.identifier.issn0968-0896
dc.identifier.lattes7501930236496670
dc.identifier.urihttp://hdl.handle.net/11449/7709
dc.identifier.wosWOS:000186134200010
dc.language.isoeng
dc.publisherElsevier B.V.
dc.relation.ispartofBioorganic & Medicinal Chemistry
dc.relation.ispartofjcr2.881
dc.relation.ispartofsjr0,871
dc.rights.accessRightsAcesso restrito
dc.sourceWeb of Science
dc.titleSynthesis and in vitro evaluation of potential antichagasic hydroxymethyinitrofurazone (NFOH-121): A new nitrofurazone prodrugen
dc.typeArtigo
dcterms.licensehttp://www.elsevier.com/about/open-access/open-access-policies/article-posting-policy
dcterms.rightsHolderElsevier B.V.
unesp.author.lattes7501930236496670
unesp.author.orcid0000-0003-4141-0455[1]
unesp.author.orcid0000-0002-7187-0818[2]
unesp.author.orcid0000-0001-5772-004X[9]
unesp.author.orcid0000-0001-7305-4673[8]
unesp.campusUniversidade Estadual Paulista (Unesp), Faculdade de Ciências Farmacêuticas, Araraquarapt
unesp.departmentCiências Biológicas - FCFpt
unesp.departmentFármacos e Medicamentos - FCFpt

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