Design, synthesis and evaluation of novel pyrazolone-4-oxadiazole for anti-inflammatory, analgesic and antipyretic activities

摘要

Compounds 2-(5-((4,5-dihydro-3-methyl-5-oxo-l-aryl-1H-pyrazol-4-yl)methylene)-1,3,4-oxadiazol-2-ylthio)-1-(4-aryl phenyl)ethanone (5 a-p) exhibited significant anti-inflammatory, analgesic and antipyretic activities. Compounds 5c and 5j exhibited significant anti-inflammatory, analgesic and antipyretic activities as compare to standard drug. The pharmacological studies revealed that the presence of electron donating groups on phenyl ring of thio ethanone side chain of 1,3,4-oxadiazol exhibited good antiinflammatory, analgesic and antipyretic activities. Molecular docking of the designed compounds with COX-2 coenzyme was found to exhibit the dock score of-3.346 to-4.716. The synthesized derivatives were characterized by spectral data.