Design and synthesis of new benzophenone derivatives with in vivo anti-inflammatory activity through dual inhibition of edema and neutrophil recruitment.

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dc.contributor.authorJanuário, Jaqueline Pereira
dc.contributor.authorSouza, Thiago Belarmino de
dc.contributor.authorLavorato, Stefânia Neiva
dc.contributor.authorMaiolini, Tatiane Cristina Silva
dc.contributor.authorDomingos, Olívia da Silva
dc.contributor.authorZanin, João Luiz Baldim
dc.contributor.authorFolquitto, Laís Regina dos Santos
dc.contributor.authorSoares, Marisi Gomes
dc.contributor.authorPaula, Daniela Aparecida Chagas de
dc.contributor.authorDias, Danielle Ferreira
dc.contributor.authorSantos, Marcelo Henrique dos
dc.date.accessioned2019-04-22T11:59:10Z
dc.date.available2019-04-22T11:59:10Z
dc.date.issued2018
dc.description.abstractA series of novel benzophenone derivatives containing a thiazole heterocyclic nucleus were designed by molecular hybridization. Molecular docking studies have demonstrated the inhibitory potential of the designed compounds against cyclooxygenase (COX) isoenzymes. These compounds were synthesized, characterized, and evaluated for their anti-inflammatory properties by the croton oil-induced ear edema assay to examine their effect on both prostaglandin (PG) production and neutrophils recruitment. The thiazole derivatives displayed a potent effect in terms of reducing ear edema. The analysis suggested that the presence of 4-phenyl-2-hydrazinothiazole and the absence of C40 -OCH3 on the benzophenone derivative structure are strongly related to the inhibition of PG production. In addition, the derivatives 2e, 3a and 3c concomitantly inhibit PG production and neutrophil recruitment, which may be a mechanism of action better than of common NSAIDs due to their inability to inhibit the neutrophil recruitment. Thus, these compounds can be considered as potential lead compounds toward the development of new anti-inflammatory drugs with an innovating mechanism of actionpt_BR
dc.identifier.citationJANUÁRIO, J. P. et al. Design and synthesis of new benzophenone derivatives with in vivo anti-inflammatory activity through dual inhibition of edema and neutrophil recruitment. Molecules, v. 23, n. 8, p. 1-23, jul. 2018. Disponível em: <https://www.mdpi.com/1420-3049/23/8/1859>. Acesso em: 7 mar. 2019.pt_BR
dc.identifier.issn1420-3049
dc.identifier.urihttp://www.repositorio.ufop.br/handle/123456789/11077
dc.language.isoen_USpt_BR
dc.rightsabertopt_BR
dc.rights.licenseThis article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/) wich permits copy and redistribute the material in any medium or format provided the original work is properly cited. Fonte: o próprio artigo.pt_BR
dc.subjectMolecular dockingpt_BR
dc.subjectHydrazinothiazolept_BR
dc.subjectTiosemicarbazonept_BR
dc.subjectEar edemapt_BR
dc.subjectStructure activity relationshippt_BR
dc.titleDesign and synthesis of new benzophenone derivatives with in vivo anti-inflammatory activity through dual inhibition of edema and neutrophil recruitment.pt_BR
dc.typeArtigo publicado em periodicopt_BR
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