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Synthesis, Analgesic and Antiinflammatory properties of Certain 5‐/6‐Acyl‐3‐(4‐substituted‐1‐piperazinylmethyl)‐2‐benzoxazolinones Derivatives
Author(s) -
Köksal Meriç,
Gökhan Nesrin,
Küpeli Esra,
Yesilada Erdem,
Erdoğan Hakkı
Publication year - 2005
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.200400937
Subject(s) - chemistry , analgesic , carrageenan , in vivo , chemical synthesis , proton nmr , stereochemistry , pharmacology , in vitro , biochemistry , medicine , microbiology and biotechnology , biology
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 ).