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  • Synthesis and characterization of some new 2(3H)-benzoxazolones with analgesic and antiinflammatory activities.

Synthesis and characterization of some new 2(3H)-benzoxazolones with analgesic and antiinflammatory activities.

Journal of enzyme inhibition and medicinal chemistry (2009-01-08)
Nesrin Gökhan-Kelekçi, Meriç Köksal, Songül Unüvar, Göknur Aktay, Hakki Erdoğan
摘要

The synthesis, characterization and pharmacological activities of a new series of (6-difluorobenzoyl)-5-methyl-3-benzoylmethyl-2(3H)-benzoxazolone and 5-methyl-3-(2-hydroxyl-2-phenylethyl)-2(3H)-benzoxazolone are described. Antiinflammatory activity was investigated by the carrageenin-induced paw oedema test and analgesic activity by acetic acid writhing and hot plate tests in mice. Among the synthesized compounds, compound 3e 6-(2,5-difluorobenzoyl)-3-(4-bromobenzoylmethyl-2(3H)-benzoxazolone was found to be the most promising compound for analgesic activity. Reduced compounds (4a-4d) displayed considerable anti-inflammatory activity compared to the other derivatives.