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 benzoxazolinones. Their chemical structures have been proven by IR, 1H-NMR and elemental analysis. Analgesic activities of these compounds were investigated by a modified Koster and constant temperature hot-plate test. Test results revealed that most of the compounds at 100 mg/kg dose level showed significant analgesic activities when compared to acetylsalicylic acid and morphine. Therefore the compounds were screened for their anti-inflammatory activities using the carrageenan hind paw edema test. Compounds 3-8 were found more active than indometacin. In gastric ulceration studies, any of the compounds showed no gastrointestinal bleeding at 100 mg/kg dose level.
Palaska
E
E
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Hacettepe University, Ankara, Turkey.
Gökhan
N
N
Erdoğan
H
H
Tel
B C
BC
Demirdamar
R
R
D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D001583:Benzoxazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D002351:Carrageenan; D004487:Edema / Q000139:chemically induced / Q000517:prevention & control; D006358:Hot Temperature; D009682:Magnetic Resonance Spectroscopy; D051379:Mice; D010147:Pain Measurement; D011930:Reaction Time / Q000187:drug effects; D013055:Spectrophotometry, Infrared; D013276:Stomach Ulcer / Q000139:chemically induced; D013329:Structure-Activity Relationship
D000894:Anti-Inflammatory Agents, Non-Steroidal; D001583:Benzoxazoles; D002351:Carrageenan