Synthesis and amelioration of inflammatory paw edema by novel benzophenone appended oxadiazole derivatives by exhibiting cyclooxygenase-2 antagonist activity - 29/05/18
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Graphical abstract |
Highlights |
• | Synthesis of benzophenone fused oxadiazole analogues 10a–j by acid amine coupling. |
• | Compounds 10a–j were subjected for HRBC membrane stabilization assay. |
• | Compound 10j was selected as potent anti-inflammatory and antiangiogenesis activity. |
• | The molecular mechanism of the compound 10j was studied by neovascularization inhibition. |
Abstract |
Ten new 2(4-hydroxy-3-benzoyl) benzamide-5-phenyl-1,3,4-oxadiazole derivatives (10a–j) were synthesized by coupling 3-benzoyl-4-hydroxybenzoic acid (5) with 2-amino-5-phenyl-1,3,4-oxadiazoles (9a–j). The structures of these compounds were confirmed by IR, 1H, 13C NMR, and mass spectra, and also by elemental analyses. The anti-inflammatory activity of the compounds 10a–j were investigated by screening them against human red blood cells (HRBC) in-vitro. The results reveal that among this series, compound 10j with hydroxy substituent, particularly at the ortho position of the phenyl ring attached to the 5th carbon atom of the oxadiazole ring possess significant membrane stabilizing activity in comparison with the control. Further, in-vivo chick chorioallantoic membrane (CAM) and rat corneal anti-angiogenesis assays were performed to assess the effect of compound 10j on endothelial cell migration. This confirmed that compound 10j inhibits the proliferation of endothelial cells. Anti-inflammatory studies detected the amelioration of carrageen induced rat hind paw edema. Further in-vivo and in-silico approaches revealed the inhibition of inflammatory marker enzyme cyclooxygenase-2 (Cox-2) and myleoperoxidase (MPO). The study reports that the compound 10j effectively act against the inflammatory mediated anti-angiogenic disorders which could be translated into a new drug in future.
El texto completo de este artículo está disponible en PDF.Keywords : Angiogenesis, Benzophenones, Inflammatory, Oxadiazoles
Esquema
Vol 103
P. 1446-1455 - juillet 2018 Regresar al númeroBienvenido a EM-consulte, la referencia de los profesionales de la salud.
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