Analgetic and antiinflammatory 7-aroylbenzofuran-5-ylacetic acids and 7-aroylbenzothiophene-5-ylacetic acids.
A number of 7-benzoylbenzofuran-5-ylacetic acids and 7-benzoylbenzothiophene-5-ylacetic acids were synthesized. The compounds were generally only 1/2 to 3 times as potent as phenylbutazone in the rat paw edema antiinflammatory assay. However, they show greater activity as analgetic agents. The most active compound is 7-[4-(methylthio)-benzoyl]benzofuran-5-ylacetic acid (5g) having 57 times the potency of aspirin in the mouse writhing analgetic assay. This compound caused virtually no gastric ulceration in rats at doses of up to 90 mg/kg.
D000085:Acetates / Q000138:chemical synthesis* / Q000494:pharmacology; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000138:chemical synthesis* / Q000494:pharmacology; D001572:Benzofurans / Q000138:chemical synthesis* / Q000494:pharmacology; D005260:Female; D008297:Male; D051379:Mice; D051381:Rats; D013329:Structure-Activity Relationship; D013876:Thiophenes / Q000138:chemical synthesis* / Q000494:pharmacology
D000085:Acetates; D000894:Anti-Inflammatory Agents, Non-Steroidal; D001572:Benzofurans; D013876:Thiophenes