Synthesis and antiinflammatory and analgesic activity of 5-aroyl-1,2-dihydro-3H-pyrrolo[1,2-a]pyrrole-1-carboxylic acids. The 6-substituted compounds.
5-Aroyl-6-substituted-1,2-dihydro-3H-pyrrolo[1,2-a]pyrrole-1-carbo xylic acids were synthesized and assayed for analgesic and antiinflammatory activity. Several of these compounds, notably the 5-(4-fluoro- and 4-chlorobenzoyl)-6-methyl derivatives 25 and 26 and the 5-(4-methyl-, 4-fluoro-, 4-chloro-, and 4-methoxybenzoyl)-6-chloro congeners 31-34 were of equal or greater potency than indomethacin as antiinflammatory and analgesic agents both in acute and chronic animal models.
D000698:Analgesia; D000818:Animals; D002264:Carboxylic Acids / Q000138:chemical synthesis / Q000627:therapeutic use; D055598:Chemical Phenomena; D002621:Chemistry; D007249:Inflammation / Q000188:drug therapy*; D009682:Magnetic Resonance Spectroscopy; D051379:Mice; D011758:Pyrroles / Q000138:chemical synthesis / Q000627:therapeutic use*; D051381:Rats; D013329:Structure-Activity Relationship
D002264:Carboxylic Acids; D011758:Pyrroles