Design, Synthesis and Pharmacological evaluation of 2,5 di phenyl 1,3,4-oxadiazole derivatives as selective COX-2 inhibitors


Vandana Jugran Negi, Ashok Kumar Sharma, Veerma Ram




A novel series of substituted-2,5-diphenyl-1,3,4-oxadiazole derivatives (3a-i) have been synthesized with the aim to get better anti-inflammatory and selective cox -2 inhibitor activity. Compound (2a-i) was reacted with several aryl acid hydrazides in phosphorousoxychloride to obtain the title compounds. Structures of the synthesized compounds were supported by means of IR, 1H NMR and mass spectroscopy.All synthesized derivatives were determined by the carrageenan induced rat paw oedema model for Anti-inflammatory activity. The entire compound gives good response for anti-inflammatory activity for this activity indomethacine was used as standard drug and compared to new synthesized drugs. Some New Synthesized drugs have to shown better activities for anti-inflammatory. Title compounds were evaluated for their anti-inflammatory and selective cox-2 activities. These compounds also exhibited significant anti-inflammatory activity, which is comparable to that of celecoxib in the carrageenan-induced rat paw edema method. The selected compounds were evaluated for their preliminary in vitro cyclooxygenase inhibitory activity against COX-2 and COX-1 enzymes. The compounds tested showed selective inhibitory activity toward COX-2(72-5%)  over COX-1 (3.5%)., amongst them compounds 3c and 3i showed appreciable COX-2 selective inhibitory activity.




1,3,4-oxadiazoles ,NSAIDs, cyclooxygenase-2 inhibitors, anti-inflammatory, rat paw edema assay.


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