Abstract

Various esters of (5,6-dimethoxy-3-oxo-2,3-dihydro-1H-inden-1-yl)acetic acid and (5-ethoxy-6-methoxy-3-oxo-2,3-dihydro-1H-inden-1-yl)acetic acid were synthesized. Anti-inflammatory and analgesic activities of these compounds were evaluated. Possibly higher lipophilicity of the ester derivatives of (5-ethoxy-6-methoxy-3-oxo-2,3-dihydro-1H-inden-1-yl)acetic acid was responsible for greater activity of these compounds compared to the esters of (5,6-dimethoxy-3-oxo-2,3-dihydro-1H-inden-1-yl)acetic acid. Compound 11d was found to be the biologically most active one. It showed 47.69% inhibition in carrageenan–induced rat paw edema in anti-inflammatory screening. It also exhibited 51.19% inhibition in acetic acid-induced writhing in analgesic screening. A few selected compounds were also screened for their antipyretic and gastrointestinal ulcerogenic potential. Promising antipyretic activity was exhibited by these compounds at the dose level of 100mg/kg p.o. These compounds also did not cause any ulceration at the highest tested dose level of 300mg/kg p.o. Experimental data indicate that better anti-inflammatory-analgesic-antipyretics can be designed using compound 11d as a lead.