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2005
Benzoxazole derivatives
R 0230
Synthesis, Analgesic and Antiinflammatory Properties of Certain 5-/6-AcylDerivatives. —
35- 139 -3-(4-substituted-1-piperazinylmethyl)-2-benzoxazolinones
The effect of molecular variation by changing the 6-acyl moiety into a 5-acyl moiety,
cf. (VIII) and (XI), on the analgesic-antiinflammatory activities is investigated. The
C-acylation of benzoxazolinone (III) is carried out taking advantage of the AlCl3/DMF
complex used as Friedel—Crafts catalyst. The acylation proceeds with satisfactory rate
and yield, only when a substrate/catalyst ratio of 11:7 is used. A classical Mannich procedure completes the reaction sequence. In vivo studies reveal that the analgesic and
antiinflammatory activities of (VIIIa) and (VIIIb) are comparable to those of Aspirin
and Indometacin. In spite of its potent activity, (VIIIc) is ulcerogenic. Less remarkable
results are obtained with compounds (XI) bearing the acyl group at 5-position of the
main ring. — (KOEKSAL, M.; GOEKHAN*, N.; KUEPELI, E.; YESILADA, E.;
ERDOGAN, H.; Arch. Pharm. (Weinheim, Ger.) 338 (2005) 2-3, 117-125; Dep.
Pharm. Chem., Fac. Pharm., Hacettepe Univ., TR-06100 Ankara, Turk.; Eng.) —
H. Hoennerscheid
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