ABSTRACT
In an attempt to minimize the gastric ulcerogenicity of 6-methoxyindan-1-acetic acid and 5,6-dimethoxyindan-1-acetic acid exhibiting high anti-inflammatory activity, we synthesized their esters, amides and nitrile derivatives. It was found that the anti-inflammatory activity of ethyl esters were almost equal to those of parent acids and phenylbutazone while other derivatives were less potent. Those ethyl esters were also found to be much less ulcerogenic than phenylbutazone.
Subject(s)
Animals , Anti-Inflammatory Agents/therapeutic use , Carrageenan/toxicity , Edema/chemically induced , Indans/analogs & derivatives , Indenes/therapeutic use , Male , Phenylbutazone/therapeutic use , Rats , Rats, Inbred Strains , Stomach Ulcer/drug therapy , Structure-Activity RelationshipABSTRACT
The anti-inflammatory activity of 6-methoxyindan-1-acetic acid (1a) and 5,6-dimethoxyindan-1-acetic acid (1b) was evaluated in various acute, subacute and chronic models of inflammation. The results of these studies suggest that they have equal or slightly more anti-inflammatory activity than phenylbutazone, a standard anti-inflammatory drug. Of the two compounds, 5,6-dimethoxyindan-l-acetic acid appeared to be slightly more active than 6-methoxyindan-l-acetic acid.