Synthesis and characterization of some new 2(3H)-benzoxazolones with analgesic and antiinflammatory activities.
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.
Gökhan-Kelekçi
Nesrin
N
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Hacettepe University, Sihhiye, Ankara, Turkey. onesrin@hacettepe.edu.tr
Köksal
Meriç
M
Unüvar
Songül
S
Aktay
Göknur
G
Erdoğan
Hakki
H
D000700:Analgesics / Q000138:chemical synthesis* / Q000494:pharmacology; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D001583:Benzoxazoles / Q000138:chemical synthesis* / Q000494:pharmacology; D004353:Drug Evaluation, Preclinical; D004487:Edema / Q000517:prevention & control; D051379:Mice; D010146:Pain / Q000517:prevention & control; D013329:Structure-Activity Relationship
D000700:Analgesics; D000893:Anti-Inflammatory Agents; D001583:Benzoxazoles; C017057:benzoxazolone