Synthesis of ibuprofen heterocyclic amides and investigation of their analgesic and toxicological properties.
A series of amides of ibuprofen with heteroaromatic amines was synthesized and assayed in vivo for their analgesic properties by means of writhing test in rats. When compared to parent ibuprofen some of the new amides exhibited a comparable or improved analgesic activity and a lower ulcerogenic effect.
Cocco
Maria Teresa
MT
Dipartimento di Tossicologia, Università degli Studi di Cagliari, Via Ospedale 72, 09124 Cagliari, Italy. tcocco@unica.it
Congiu
Cenzo
C
Onnis
Valentina
V
Morelli
Micaela
M
Cauli
Omar
O
D019342:Acetic Acid / Q000037:antagonists & inhibitors / Q000633:toxicity; D000284:Administration, Oral; D000577:Amides / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity*; D018712:Analgesics, Non-Narcotic / Q000737:chemistry* / Q000633:toxicity*; D000818:Animals; D007052:Ibuprofen / Q000031:analogs & derivatives* / Q000494:pharmacology / Q000633:toxicity; D007274:Injections, Intraperitoneal; D009682:Magnetic Resonance Spectroscopy; D008297:Male; D010146:Pain / Q000139:chemically induced; D010147:Pain Measurement / Q000187:drug effects / Q000379:methods; D011726:Pyridinium Compounds / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity*; D051381:Rats; D017207:Rats, Sprague-Dawley; D013055:Spectrophotometry, Infrared; D013276:Stomach Ulcer / Q000517:prevention & control; D013329:Structure-Activity Relationship
D000577:Amides; D018712:Analgesics, Non-Narcotic; D011726:Pyridinium Compounds; D019342:Acetic Acid; D007052:Ibuprofen