1610601-59-6Relevant articles and documents
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 anti-inflammatory activity
Bansal, Sumit,Bala, Manju,Suthar, Sharad Kumar,Choudhary, Shivani,Bhattacharya, Shoumyo,Bhardwaj, Varun,Singla, Sumit,Joseph, Alex
, p. 167 - 174 (2014/05/20)
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 IC of 0.31 μM showing promising degree of anti-inflammatory activity in the carrageenan-induced rat paw edema model with ED of 74.3 mg/kg. The lead compound 9g further showed suppression of acetic acid-induced writhes comparable to that of aspirin and gastro-sparing profile superior to the aspirin. Molecular docking analysis displayed higher binding affinity of ligands towards COX-2 than COX-1.