Synthesis and biological evaluation of amide derivatives of (5,6-dimethoxy-2,3-dihydro-1H-inden-1-yl)acetic acid as anti-inflammatory agents with reduced gastrointestinal ulcerogenecity

A variety of amide derivatives of (5,6-dimethoxy-2,3-dihydro-1H-inden-1-yl)acetic acid were synthesized and screened for their analgesic and anti-inflammatory activities. The compounds were found to have longer activity profile exceeding that of indomethacin in carrageenaninduced rat paw edema model. Few selected compounds were also screened for their antipyretic, anti-arthritic and ulcerogenecity potential. From these studies it can be concluded that these compounds though have significant antipyretic activity did not act through the inhibition of TNF-alpha. The test compounds failed to prevent the development of secondary inflammation in adjuvant-induced arthritis assay. However, these compounds showed no ulcer formation at the tested dose level of 100 mg/kg p.o. (C) 2007 Elsevier Masson SAS. All rights reserved.