Synthesis, ex Vivo and in Vitro Hydrolysis Study of an Indoline Derivative Designed as an Anti-Inflammatory with Reduced Gastric Ulceration Properties

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dc.contributor.authorChin, Chung Man [UNESP]
dc.contributor.authordos Santos, Jean Leandro [UNESP]
dc.contributor.authorOliveira, Ednir Vizioli [UNESP]
dc.contributor.authorBlau, Lorena [UNESP]
dc.contributor.authorMenegon, Renato Farina [UNESP]
dc.contributor.authorPeccinini, Rosangela Goncalves [UNESP]
dc.contributor.institutionUniversidade Estadual Paulista (Unesp)
dc.date.accessioned2014-05-20T13:24:46Z
dc.date.available2014-05-20T13:24:46Z
dc.date.issued2009-09-01
dc.description.abstractThe compound 1-(2,6-dichlorophenyl)indolin-2-one (1), planned as a pro-drug of diclofenac (2), was easily synthesized in 94% yield by an intramolecular reaction in the presence of coupling agent (i.e., EDC). Compound 1 showed anti-inflammatory and analgesic activity without gastro-ulcerogenic effects. The chemical and enzymatic hydrolysis profile of the lactam derivative 1 does not indicate conversion to diclofenac (2). This compound is a new non-ulcerogenic prototype for treatment of chronic inflammatory diseases.en
dc.description.affiliationUNESP, Fac Ciencias Farmaceut, Dept Farmacos & Medicamentos, Lapdesf Lab Pesquisa & Desenvolvimento Farmacos, BR-14801902 Araraquara, SP, Brazil
dc.description.affiliationUNESP, Fac Ciencias Farmaceut, Dept Principios Ativos Nat & Toxicol, BR-14801902 Araraquara, SP, Brazil
dc.description.affiliationUnespUNESP, Fac Ciencias Farmaceut, Dept Farmacos & Medicamentos, Lapdesf Lab Pesquisa & Desenvolvimento Farmacos, BR-14801902 Araraquara, SP, Brazil
dc.description.affiliationUnespUNESP, Fac Ciencias Farmaceut, Dept Principios Ativos Nat & Toxicol, BR-14801902 Araraquara, SP, Brazil
dc.description.sponsorshipCoordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)
dc.description.sponsorshipFundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)
dc.description.sponsorshipIdFAPESP: 07/56115-0
dc.format.extent3187-3197
dc.identifierhttp://dx.doi.org/10.3390/molecules14093187
dc.identifier.citationMolecules. Basel: Molecular Diversity Preservation International-mdpi, v. 14, n. 9, p. 3187-3197, 2009.
dc.identifier.doi10.3390/molecules14093187
dc.identifier.fileWOS000270201900007.pdf
dc.identifier.issn1420-3049
dc.identifier.lattes9734333607975413
dc.identifier.lattes1066743423929093
dc.identifier.orcid0000-0003-4141-0455
dc.identifier.urihttp://hdl.handle.net/11449/7781
dc.identifier.wosWOS:000270201900007
dc.language.isoeng
dc.publisherMolecular Diversity Preservation International-mdpi
dc.relation.ispartofMolecules
dc.relation.ispartofjcr3.098
dc.relation.ispartofsjr0,855
dc.rights.accessRightsAcesso aberto
dc.sourceWeb of Science
dc.subjectindolinoneen
dc.subjectpro-drugen
dc.subjectanti-inflammatoryen
dc.subjecthydrolysisen
dc.subjectdiclofenacen
dc.titleSynthesis, ex Vivo and in Vitro Hydrolysis Study of an Indoline Derivative Designed as an Anti-Inflammatory with Reduced Gastric Ulceration Propertiesen
dc.typeArtigo
dcterms.licensehttp://www.mdpi.com/about/openaccess
dcterms.rightsHolderMolecular Diversity Preservation International-mdpi
unesp.author.lattes1066743423929093
unesp.author.lattes9734333607975413[1]
unesp.author.orcid0000-0003-4141-0455[1]
unesp.campusUniversidade Estadual Paulista (Unesp), Faculdade de Ciências Farmacêuticas, Araraquarapt

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Artigos - Fármacos e Medicamentos - FCFAR
Artigos - Princípios Ativos Naturais e Toxicologia - FCFAR