Novel antiinflammatory analgesics: 3-(2-/4-pyridylethyl)-benzoxazolinone and oxazolo[4,5-b]pyridin-2-one derivatives

Gökhan N., Erdogan H., Durlu T., Demirdamar R.

ARCHIV DER PHARMAZIE, vol.332, no.2, pp.43-49, 1999 (SCI-Expanded) identifier identifier identifier

  • Publication Type: Article / Article
  • Volume: 332 Issue: 2
  • Publication Date: 1999
  • Journal Name: ARCHIV DER PHARMAZIE
  • Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Page Numbers: pp.43-49
  • Keywords: 2-benzoxazolinone, oxazolo[4,5-b]pyridin-2-one, acylation, pyridylethyl, analgesic-antiinflammatory activity, DRUGS
  • Hacettepe University Affiliated: Yes

Abstract

Twenty-two new 3-[2-(2- and/or 4-pyridyl)ethyl] benzoxazolinone and oxazolo[4,5-b]pyridin-2-one derivatives have been synthesized by reacting 2- and/or 4-vinylpyridine and appropriate benzoxazolinones and oxazolo[4,5-b]pyridine-2-one. Their chemical structures have been proven by IR, H-1-NMR,C-13-NMR, mass spectroscopy, and elemental analysis. The analgesic activities of these compounds were investigated by a modified Koster's Test. Test results revealed that, at 100 mg/kg dose level, most of the compounds showed significant analgesic activities when compared pared to aspirin. Therefore the compounds were screened for their antiinflammatory activities using the carrageenan hind paw edema test. Compounds 1, 7, 10, 11, 12, 13, 15, 18, 20, 21 were found more active than indomethacine. In gastric ulceration studies gastrointestinal bleeding was not observed at 100 mg/kg dose level in 1 and 2.