title: Synthesis, analgesic and antiinflammatory properties of certain 5-/6-acyl-3-(4-substituted-1-piperazinylmethyl)-2-benzoxazolinones derivatives.
abstract: The synthesis of a novel series of Mannich bases of 5-/6-acyl-5-methyl-2-benzoxazolinones has been described. The structures attributed to compounds 2a, 3a, 4a, 4b, 9a, 9b, 5a-5g, 6a-6g, 10a, 10g, 11a, 11g have been elucidated using IR and (1)H NMR spectroscopic techniques besides elemental analysis. The compounds have been evaluated for their in vivo analgesic and antiinflammatory activities using the p-benzoquinone-induced writhing test and the carrageenan hind paw oedema test in mice, respectively. In addition, the ulcerogenic effects of the compounds were determined. Among the tested derivatives most promising results were obtained for the compounds bearing a 6-(4-chlorobenzoyl) at C-6 position and 2-/4-fluorophenyl at C-3 position of 2-benzoxazolinone ring (11c, 11d).
authors.affiliation: Yeditepe University, Faculty of Pharmacy, Istanbul, Turkey.
authors.forename: Meriç
authors.initials: M
authors.lastname: Köksal
authors.forename: Nesrin
authors.initials: N
authors.lastname: Gökhan
authors.forename: Esra
authors.initials: E
authors.lastname: Küpeli
authors.forename: Erdem
authors.initials: E
authors.lastname: Yesilada
authors.forename: Hakki
authors.initials: H
authors.lastname: Erdoğan
mesh_terms: D000700:Analgesics / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D001583:Benzoxazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D008297:Male; D051379:Mice; D010147:Pain Measurement; D013329:Structure-Activity Relationship
chemical_list: D000700:Analgesics; D000893:Anti-Inflammatory Agents; D001583:Benzoxazoles