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

dc.creatorSantos, Marcelo H. dos
dc.creatorJanuario, Jaqueline P.
dc.creatorSouza, Thiago B. de
dc.creatorLavorato, Stefânia N.
dc.creatorMaiolini, Tatiane C. S.
dc.creatorDomingos, Olívia S.
dc.creatorBaldim, João L.
dc.creatorFolquitto, Laís R. S.
dc.creatorSoares, Marisi G.
dc.creatorChagas-Paula, Daniela A.
dc.creatorDias, Danielle F.
dc.date2019-03-08T11:57:45Z
dc.date2019-03-08T11:57:45Z
dc.date2018-08
dc.date.accessioned2023-09-27T21:52:25Z
dc.date.available2023-09-27T21:52:25Z
dc.identifier14203049
dc.identifierhttps://doi.org/10.3390/molecules23081859
dc.identifierhttp://www.locus.ufv.br/handle/123456789/23831
dc.identifier.urihttps://repositorioslatinoamericanos.uchile.cl/handle/2250/8967408
dc.descriptionA 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 C4 0 -OCH 3 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 action.
dc.formatpdf
dc.formatapplication/pdf
dc.languageeng
dc.publisherMolecules
dc.relationVolume 23, Number 08, Article 1859, Pages 01- 23, August 2018
dc.rightsOpen Access
dc.subjectHydrazinothiazole
dc.subjectTiosemicarbazone
dc.subjectMolecular docking
dc.subjectStructure activity relationship
dc.subjectEar edema
dc.titleDesign and synthesis of new Benzophenone derivatives with in vivo anti-inflammatory activity through dual inhibition of edema and neutrophil recruitment
dc.typeArtigo


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