Abstract
A series of 2-trifluoromethyl/sulfonamido-5,6-diarylsubstituted imidazo[2,1-
b]-1,3,4-thiadiazole derivatives
15a–
j have been synthesized by the reaction of 2-amino-5-trifluoromethyl/sulfonamido-1,3,4-thiadiazoles
14a–
b and appropriately substituted α-bromo-1,2-(
p-substituted)diaryl-1-ethanones
13a–
h. Structures of these compounds were established by IR,
1H NMR,
13C NMR, Mass, and HRMS data. The selected compounds were evaluated for their preliminary in vitro cyclooxygenase inhibitory activity against COX-2 and COX-1enzymes using colorimetric method. The compounds tested showed selective inhibitory activity toward COX-2 (80.6–49.4%) over COX-1 (30.6–8.6), amongst them compounds
15f and
15j showed appreciable COX-2 selective inhibitory activity. These compounds also exhibited significant anti-inflammatory activity (70.09–42.32%), which is comparable to that of celecoxib in the carrageenan-induced rat paw edema method.