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 carrageenan-induced 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-α. 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.

Graphical abstractA series of (5,6-dimethoxy-2,3-dihydro-1H-inden-1-yl)acetic acid amides were synthesized and screened for their anti-inflammatory and related biological activities. The synthesized compounds showed long duration of anti-inflammatory activity and were free from ulcerogenecity liability of common NSAIDs.Figure optionsDownload full-size imageDownload as PowerPoint slide