Pharmacological evaluation and preparation of nonsteroidal anti-inflammatory drugs containing an N-Acyl hydrazone subunit

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dc.contributor.authorMelo, Thais Regina Ferreira de [UNESP]
dc.contributor.authorChelucci, Rafael Consolin [UNESP]
dc.contributor.authorPires, Maria Elisa Lopes [UNESP]
dc.contributor.authorDutra, Luiz Antonio [UNESP]
dc.contributor.authorBarbieri, Karina Pereira [UNESP]
dc.contributor.authorBosquesi, Priscila Longhin [UNESP]
dc.contributor.authorTrossini, Gustavo Henrique Goulart
dc.contributor.authorChung, Man Chin [UNESP]
dc.contributor.authorSantos, Jean Leandro dos [UNESP]
dc.contributor.institutionUniversidade Estadual Paulista (Unesp)|Universidade de São Paulo (USP)
dc.date.accessioned2016-01-28T16:56:29Z
dc.date.available2016-01-28T16:56:29Z
dc.date.issued2014
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.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.format.extent5821-5837
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.doi10.3390/ijms15045821
dc.identifier.fileISSN1422-0067-2014-15-04-5821-5837.pdf
dc.identifier.issn1422-0067
dc.identifier.lattes5178218874772717
dc.identifier.lattes9734333607975413
dc.identifier.lattes5737933639516944
dc.identifier.orcid0000-0003-4141-0455
dc.identifier.urihttp://hdl.handle.net/11449/133754
dc.language.isoeng
dc.relation.ispartofInternational Journal of Molecular Sciences
dc.relation.ispartofjcr3.687
dc.relation.ispartofsjr1,260
dc.rights.accessRightsAcesso aberto
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.typeArtigo
unesp.author.lattes5178218874772717
unesp.author.lattes5737933639516944
unesp.author.lattes9734333607975413[8]
unesp.author.orcid0000-0003-4141-0455[8]
unesp.campusUniversidade Estadual Paulista (Unesp), Faculdade de Ciências Farmacêuticas, Araraquarapt
unesp.departmentFármacos e Médicamentospt

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