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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Date
2018
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Abstract
A 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 action
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Keywords
Molecular docking, Hydrazinothiazole, Tiosemicarbazone, Ear edema, Structure activity relationship
Citation
JANUÁRIO, 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.