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

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/o r 4-vinylpyridine and appropriate benzoxazolinones and oxazolo[4,5-b]pyridi ne-2-one. Their chemical structures have been proven by IR, H-1-NMR,C-13-NM R, mass spectroscopy, and elemental analysis. The analgesic activities of t hese compounds were investigated by a modified Koster's Test. Test results revealed that, at 100 mg/kg dose level, most of the compounds showed signif icant analgesic activities when compared pared to aspirin. Therefore the co mpounds were screened for their antiinflammatory activities using the carra geenan 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 ga strointestinal bleeding was not observed at 100 mg/kg dose level in 1 and 2 .