SOME NEW BENZOXAZOLINONE DERIVATIVES WITH ANALGESIC AND ANTIINFLAMMATORY ACTIVITIES

Fourteen new 6-acyl-2-benzoxazolinone, ethyl-(6-acyl-2-benzoxazolinone )acetate and (6-acyl-2-benzoxazolinone-3-yl) acetic acid derivatives w ere synthesized, and their physical properties and UV absorption data were determined. Their chemical structures were elucidated by IR, H-1- NMR and elemental analysis. The analgesic activities of these compound s were investigated by a modified Koster's test. It was shown that the respective activities of compounds 1-4 and 10-14 were higher than tha t of acetylsalicylic acid. Therefore, they were screened for additiona lly anti-inflammatory activities using the carrageenan mouse paw edema test. The compounds were further screened for their ability to inhibi t prostaglandin E2 (PGE2) induced paw edema and compared to indometaci n. Compounds 12 and 13 were very potent in inhibiting PGE2 induced ede ma.