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dc.contributor.authorMelo, Thais Regina Ferreira de-
dc.contributor.authorChelucci, Rafael Consolin-
dc.contributor.authorPires, Maria Elisa Lopes-
dc.contributor.authorDutra, Luiz Antonio-
dc.contributor.authorBarbieri, Karina Pereira-
dc.contributor.authorBosquesi, Priscila Longhin-
dc.contributor.authorTrossini, Gustavo Henrique Goulart-
dc.contributor.authorChung, Man Chin-
dc.contributor.authorSantos, Jean Leandro dos-
dc.date.accessioned2016-01-28T16:56:29Z-
dc.date.accessioned2016-10-25T21:28:48Z-
dc.date.available2016-01-28T16:56:29Z-
dc.date.available2016-10-25T21:28:48Z-
dc.date.issued2014-
dc.identifierhttp://dx.doi.org/10.3390/ijms15045821-
dc.identifier.citationInternational Journal of Molecular Sciences, v. 15, n. 4, p. 5821-5837, 2014.-
dc.identifier.issn1422-0067-
dc.identifier.urihttp://hdl.handle.net/11449/133754-
dc.identifier.urihttp://acervodigital.unesp.br/handle/11449/133754-
dc.description.abstractA series of anti-inflammatory derivatives containing an N-acyl hydrazone subunit (4a–e) were synthesized and characterized. Docking studies were performed that suggest that compounds 4a–e bind to cyclooxygenase (COX)-1 and COX-2 isoforms, but with higher affinity for COX-2. The compounds display similar anti-inflammatory activities in vivo, although compound 4c is the most effective compound for inhibiting rat paw edema, with a reduction in the extent of inflammation of 35.9% and 52.8% at 2 and 4 h, respectively. The anti-inflammatory activity of N-acyl hydrazone derivatives was inferior to their respective parent drugs, except for compound 4c after 5 h. Ulcerogenic studies revealed that compounds 4a–e are less gastrotoxic than the respective parent drug. Compounds 4b–e demonstrated mucosal damage comparable to celecoxib. The in vivo analgesic activities of the compounds are higher than the respective parent drug for compounds 4a–b and 4d–e. Compound 4a was more active than dipyrone in reducing acetic-acid-induced abdominal constrictions. Our results indicate that compounds 4a–e are anti-inflammatory and analgesic compounds with reduced gastrotoxicity compared to their respective parent non-steroidal anti-inflammatory drugs.en
dc.format.extent5821-5837-
dc.language.isoeng-
dc.sourceCurrículo Lattes-
dc.subjectAnti-inflammatoryen
dc.subjectAnalgesicen
dc.subjectHydrazoneen
dc.subjectMolecular hybridizationen
dc.subjectNon-steroidalen
dc.subjectAnti-inflammatoryen
dc.subjectNSAIDen
dc.subjectDockingen
dc.subjectMolecular modelingen
dc.subjectCOXen
dc.titlePharmacological evaluation and preparation of nonsteroidal anti-inflammatory drugs containing an N-Acyl hydrazone subuniten
dc.typeoutro-
dc.contributor.institutionUniversidade Estadual Paulista (UNESP)|Universidade de São Paulo (USP)-
dc.description.affiliationUniversidade Estadual Paulista Júlio de Mesquita Filho, Departamento de Fármacos e Médicamentos, Faculdade de Ciências Farmacêuticas de Araraquara, Araraquara, Rodovia Araraquara-Jaú Km. 01, Campus Ville, CEP 14801902, SP, Brasil-
dc.description.affiliationFaculty of Pharmaceutical Science, University of São Paulo, Av. Professor Lineu Prestes 580, São Paulo 05508-900, SP, Brazil-
dc.description.affiliationUnespUniversidade Estadual Paulista Júlio de Mesquita Filho, Departamento de Fármacos e Médicamentos, Faculdade de Ciências Farmacêuticas de Araraquara, Araraquara, Rodovia Araraquara-Jaú Km. 01, Campus Ville, CEP 14801902, SP, Brasil-
dc.identifier.doi10.3390/ijms15045821-
dc.rights.accessRightsAcesso aberto-
dc.identifier.fileISSN1422-0067-2014-15-04-5821-5837.pdf-
dc.relation.ispartofInternational Journal of Molecular Sciences-
dc.identifier.lattes5737933639516944-
dc.identifier.lattes5178218874772717-
Appears in Collections:Artigos, TCCs, Teses e Dissertações da Unesp

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