Synthesis of some new pyridyl-ethylated benzoxazolinones with analgesic and anti-inflammatory activities

Twelve new 3-[2-(2- and/or 4-pyridyl)ethyl]benzoxazolinone derivatives have been synthesized by reacting 2- and/or 4-vinylpyridine and appropriate ben zoxazolinones. Their chemical structures have been proven by IR, H-1-NMR an d elemental analysis. Analgesic activities of these compounds were investig ated by a modified Koster and constant temperature hot-plate test. Test res ults revealed that most of the compounds at 100 mg/kg dose level showed sig nificant analgesic activities when compared to acetylsalicylic acid and mor phine. Therefore the compounds were screened for their anti-inflammatory ac tivities using the carrageenan hind paw edema test. Compounds 3-8 were foun d more active than indometacin. In gastric ulceration studies, any of the c ompounds showed no gastrointestinal bleeding at 100 mg/kg dose level.