Indeno[1,2-c]pyrazolone acetic acids as semirigid analogues of the nonsteroidal anti-inflammatory drugs.
A series of 3-substituted indeno[1,2-c]pyrazol-4(1H)-one-2-acetic acids (3a-e) and 3-substituted indeno[1,2-c]pyrazol-4(1H)-one-1-acetic acids (4a-e) were synthesized as semirigid analogues of tolmetin (1). These compounds were evaluated for their anti-inflammatory action by investigating their ability to block arachidonic acid metabolism in vitro as well as the ability to block carrageenan-induced rat foot edema in vivo. No consistent pattern of biological activity was noted.
Lemke
T L
TL
Department of Medicinal Chemistry, College of Pharmacy, University of Houston, TX 77004.
Abebe
E
E
Moore
P F
PF
Carty
T J
TJ
D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000138:chemical synthesis*; D001095:Arachidonic Acids / Q000378:metabolism; D055598:Chemical Phenomena; D002621:Chemistry; D004487:Edema / Q000378:metabolism / Q000517:prevention & control; D007192:Indenes / Q000138:chemical synthesis* / Q000494:pharmacology; D007942:Leukemia, Experimental / Q000378:metabolism; D008297:Male; D011451:Prostaglandin-Endoperoxide Synthases / Q000378:metabolism; D011720:Pyrazoles / Q000138:chemical synthesis* / Q000494:pharmacology; D051381:Rats; D011919:Rats, Inbred Strains; D014407:Tumor Cells, Cultured / Q000187:drug effects / Q000378:metabolism
D000894:Anti-Inflammatory Agents, Non-Steroidal; D001095:Arachidonic Acids; D007192:Indenes; D011720:Pyrazoles; D011451:Prostaglandin-Endoperoxide Synthases