Synthesis and Characterization of Novel IMIDAZO[1,2- A]Pyridine Derivatives as Potential CYCLOOXYGENASE-2 (COX-2) Inhibitors (original) (raw)

Towards the development of selective cyclooxygenase-2 inhibitors, a series of imidazo[1,2-a]pyridine derivatives is described. All the compounds containing sulfonamide, nitrile, acid, amide and aldehyde functionalities were computationally screened and binding affinity scores for all synthesized compounds with COX-1 and COX-2 were compared. The computational observations showed, three top ranked compounds (26, 15 and 22) having selectively more affinity for COX2. These were selected for pharmacological evaluation using carrageenan-induced rat paw oedema model. Compound 26 showed maximum activity (52.90%) which was closer to standard drug indomethacin (54.66%). The safety parameter of the potent compound (26) was assessed using aspirin induced gastric ulceration animal model.