Studies on novel 7-acyl-5-chloro-2-oxo-3H-benzoxazole derivatives as potential analgesic and anti-inflammatory agents.
In this study, a series of (7-acyl-5-chloro-2-oxo-3H-benzoxazol-3-yl)alkanoic acid derivatives were synthesized and evaluated for their analgesic and anti-inflammatory activities by using the p-benzoquinone-induced writhing test and the carrageenan hind paw edema model, respectively. Acetic acid-induced peritoneal capillary permeability test and serotonin-induced hind paw edema test were also employed for the most active compounds. The test results indicated that (7-acyl-2-oxo-3H-benzoxazol-3-yl)alkanoic acids (Compounds 6 a-c, 8 a-c, 10 a-c) were equally or more potent analgesic and anti-inflammatory agents than aspirin and indomethacin respectively. The compounds 8a and 8c, but not 8b have the longest carbon chain on alkanoic acid moiety did not induce gastric lesion in mice.
Unlü
Serdar
S
Department of Pharmaceutical Chemistry, Division of Pharmaceutical Sciences, Faculty of Pharmacy, Gazi University, Ankara, Turkey. sunlu@gazi.edu.tr
Baytas
Sultan Nacak
SN
Kupeli
Esra
E
Yesilada
Erdem
E
D000700:Analgesics / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D001241:Aspirin / Q000494:pharmacology; D001583:Benzoxazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D002199:Capillary Permeability / Q000187:drug effects; D002351:Carrageenan; D015195:Drug Design; D004487:Edema / Q000139:chemically induced / Q000188:drug therapy; D007213:Indomethacin / Q000494:pharmacology; D007249:Inflammation / Q000188:drug therapy / Q000378:metabolism; D051379:Mice; D010147:Pain Measurement; D023382:Toxicity Tests, Acute
D000700:Analgesics; D000894:Anti-Inflammatory Agents, Non-Steroidal; D001583:Benzoxazoles; D002351:Carrageenan; D001241:Aspirin; D007213:Indomethacin