Anti-inflammatory derivatives of indan-1-acetic acids with low gastric irritancy.
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.
D000818:Animals; D000893:Anti-Inflammatory Agents / Q000627:therapeutic use*; D002351:Carrageenan / Q000633:toxicity; D004487:Edema / Q000139:chemically induced / Q000188:drug therapy; D007189:Indans / Q000031:analogs & derivatives* / Q000627:therapeutic use*; D007192:Indenes / Q000627:therapeutic use*; D008297:Male; D010653:Phenylbutazone / Q000627:therapeutic use; D051381:Rats; D011919:Rats, Inbred Strains; D013276:Stomach Ulcer / Q000188:drug therapy*; D013329:Structure-Activity Relationship
D000893:Anti-Inflammatory Agents; D007189:Indans; D007192:Indenes; C036583:6-methoxyindan-1-acetic acid; C036584:5,6-dimethoxyindan-1-acetic acid; D002351:Carrageenan; D010653:Phenylbutazone