Microwave assisted synthesis,pharmacological activities,and molecular docking studies of ethyl 2-[2-substituted-4-(Thiophenyl) thiazolyl] acetates

A series of ethyl 2-[2-arylamino-4-(thiophen-2-yl) thiazol-5-yl] acetates (5a-5k) and ethyl 2-[2-(arylhydrazino)-4-(thiophen-2-yl) thiazol-5-yl] acetates (9a-9g) were synthesized and screened for their anti-inflammatory,analgesic,and antioxidant activities. in-vivo test results showed that the compounds with halogen substitution (5c,5g,5h,5i and 5j) at the para position on the 2-aryl amino group exhibited good anti-inflammatory and analgesic activities,similar to that of indomethacin and aspirin,respectively. the ethyl 2-[2-(arylhydrazino)-4-(thiophen-2-yl) thiazol-5-yl] acetates (9a-9g) showed better anti-oxidant activity than compounds 5a-5k,comparable to ascorbic acid. however,these compounds showed moderate to weak anti-inflammatory and analgesic activities. further,a molecular docking study was performed to predict the possible binding modes on cyclooxygenase-1 (cox-1) and cox-2 for the tested compounds. good correlation was observed between the anti-inflammatory activity of the compounds and the results of the binding modes in cox-2. © 2017 by school of pharmacy shaheed beheshti university of medical sciences and health services.