Synthesis and in vitro evaluation of potential antichagasic hydroxymethyinitrofurazone (NFOH-121): A new nitrofurazone prodrug
dc.contributor.author | Chung, M. C. | |
dc.contributor.author | Guido, RVC | |
dc.contributor.author | Martinelli, T. F. | |
dc.contributor.author | Goncalves, M. F. | |
dc.contributor.author | Polli, M. C. | |
dc.contributor.author | Botelho, KCA | |
dc.contributor.author | Varanda, Eliana Aparecida [UNESP] | |
dc.contributor.author | Colli, W. | |
dc.contributor.author | Miranda, MTM | |
dc.contributor.author | Ferreira, E. I. | |
dc.contributor.institution | Universidade de São Paulo (USP) | |
dc.contributor.institution | Universidade Estadual Paulista (Unesp) | |
dc.date.accessioned | 2014-05-20T13:24:38Z | |
dc.date.available | 2014-05-20T13:24:38Z | |
dc.date.issued | 2003-11-03 | |
dc.description.abstract | The 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.affiliation | USP, Dept Farm, Fac Ciências Farmaceut, BR-05389970 São Paulo, Brazil | |
dc.description.affiliation | UNESP, Lapdesf Lab Pesquisa & Desenvolvimento Farm, Dept Farmacos & Med, Fac Ciências Farmaceut, BR-14801902 Araraquara, SP, Brazil | |
dc.description.affiliation | UNESP, Dept Ciências Biol, Fac Ciências Farmaceut, BR-14801902 Araraquara, SP, Brazil | |
dc.description.affiliationUnesp | UNESP, Lapdesf Lab Pesquisa & Desenvolvimento Farm, Dept Farmacos & Med, Fac Ciências Farmaceut, BR-14801902 Araraquara, SP, Brazil | |
dc.description.affiliationUnesp | UNESP, Dept Ciências Biol, Fac Ciências Farmaceut, BR-14801902 Araraquara, SP, Brazil | |
dc.format.extent | 4779-4783 | |
dc.identifier | http://dx.doi.org/10.1016/j.bmc.2003.07.004 | |
dc.identifier.citation | Bioorganic & Medicinal Chemistry. Oxford: Pergamon-Elsevier B.V., v. 11, n. 22, p. 4779-4783, 2003. | |
dc.identifier.doi | 10.1016/j.bmc.2003.07.004 | |
dc.identifier.issn | 0968-0896 | |
dc.identifier.lattes | 7501930236496670 | |
dc.identifier.uri | http://hdl.handle.net/11449/7709 | |
dc.identifier.wos | WOS:000186134200010 | |
dc.language.iso | eng | |
dc.publisher | Elsevier B.V. | |
dc.relation.ispartof | Bioorganic & Medicinal Chemistry | |
dc.relation.ispartofjcr | 2.881 | |
dc.relation.ispartofsjr | 0,871 | |
dc.rights.accessRights | Acesso restrito | |
dc.source | Web of Science | |
dc.title | Synthesis and in vitro evaluation of potential antichagasic hydroxymethyinitrofurazone (NFOH-121): A new nitrofurazone prodrug | en |
dc.type | Artigo | |
dcterms.license | http://www.elsevier.com/about/open-access/open-access-policies/article-posting-policy | |
dcterms.rightsHolder | Elsevier B.V. | |
unesp.author.lattes | 7501930236496670 | |
unesp.author.orcid | 0000-0003-4141-0455[1] | |
unesp.author.orcid | 0000-0002-7187-0818[2] | |
unesp.author.orcid | 0000-0001-5772-004X[9] | |
unesp.author.orcid | 0000-0001-7305-4673[8] | |
unesp.campus | Universidade Estadual Paulista (Unesp), Faculdade de Ciências Farmacêuticas, Araraquara | pt |
unesp.department | Ciências Biológicas - FCF | pt |
unesp.department | Fármacos e Medicamentos - FCF | pt |
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