Studies on novel 7-acyl-5-chloro-2-oxo-3H-benzoxazole derivatives as potential analgesic and anti-inflammatory agents

Unlu S., BAYTAŞ S., Kupeli E., Yesilada E.

ARCHIV DER PHARMAZIE, vol.336, pp.310-321, 2003 (Peer-Reviewed Journal) identifier identifier identifier

  • Publication Type: Article / Article
  • Volume: 336
  • Publication Date: 2003
  • Doi Number: 10.1002/ardp.200300748
  • Journal Indexes: Science Citation Index Expanded, Scopus
  • Page Numbers: pp.310-321
  • Keywords: 7-acyl-2-oxo-3H-benzoxazoles, alkanoic acids, propionitriles, QSAR, analgesic and anti-inflammatory activity, 6-ACYL BENZOXAZOLINONES, MOUSE, ACIDS, MICE, RATS


In this study, a series of (7-acyl-5-chloro-2-oxo-3H-benzoxazol-3-yl)alkanoic acid derivatives were synthesized and evaluated for their analgesic and anti-inflammatory activities by using the p-benzoquinone-induced writhing test and the carrageenan hind paw edema model, respectively. Acetic acid-induced peritoneal capillary permeability test and serotonin-induced hind paw edema test were also employed for the most active compounds. The test results indicated that (7-acyl-2-oxo-3H-benzoxazol-3-yl)alkanoic acids (Compounds 6 a-c, 8 a-c, 10 a-c) were equally or more potent analgesic and anti-inflammatory agents than aspirin and indomethacin respectively. The compounds 8 a and 8 c, but not 8 b which have the longest carbon chain on alkanoic acid moiety did not induce gastric lesion in mice.