Suthar, Sharad Kumar and Joseph, Alex (2014) Design and synthesis of novel 2-phenyl-5-(1,3-diphenyl-1H-pyrazol- 4-yl)-1,3,4-oxadiazoles as selective COX-2 inhibitors with potent antiinflammatory activity. European Journal of Medicinal Chemistry, 80. pp. 167-174. ISSN 0223-5234

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Abstract

A novel series of 2-phenyl-5-(1,3-diphenyl-1H-pyrazol-4-yl)-1,3,4-oxadiazoles were designed and synthesized for selective COX-2 inhibition with potent anti-inflammatory activity. Among the compounds tested, 9g (2-(3-(4-nitrophenyl)-1-phenyl-1H-pyrazol-4-yl)-5-phenyl-1,3,4-oxadiazole) was found to be the most potent inhibitor of COX-2 with IC50 of 0.31 mM showing promising degree of anti-inflammatory activity in the carrageenan-induced rat paw edema model with ED50 of 74.3 mg/kg. The lead compound 9g further showed suppression of acetic acid-induced writhes comparable to that of aspirin and gastrosparing profile superior to the aspirin. Molecular docking analysis displayed higher binding affinity of ligands towards COX-2 than COX-1.

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