Abstract

SYNTHESIS AND CHARACTERIZATION OF NOVEL IMIDAZO[1,2-A]PYRIDINE DERIVATIVES AS POTENTIAL CYCLOOXYGENASE-2 (COX-2) INHIBITORS

Shivaji S. Pandit*

ABSTRACT

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 COX-2. 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.

Keywords: Imidazo[1,2-a]pyridine; Cyclooxygenase-2; Docking study; carrageenan-induced rat paw oedema model; gastric ulceration animal model.