Erol D D, Demirdamar R, Duru S
Pharmaceutical Chemistry Department, Faculty of Pharmacy, Hacettepe University, Ankara, Turkey.
J Pharm Sci. 1994 Mar;83(3):273-5. doi: 10.1002/jps.2600830302.
6-Acyl-2(3H)-benzoxazolone derivatives were reacted with 4-substituted phenacyl bromide in ethanol to give the corresponding 6-acyl-3-[(4-substitutedbenzoyl)methyl]-2(3H)-benzoxazolones . The compounds were screened for their analgesic, antiinflammatory activities. The eight compounds synthesized showed high analgesic activities and further investigation revealed compounds 3, 6 and 7 to be potent inhibitors of carrageenan- and arachidonic acid-induced paw edema. The PGE2 isolated from the carrageenan paw edema fluid was also significantly low in mice treated with compounds 3, 6 and 7.
6-酰基-2(3H)-苯并恶唑酮衍生物与4-取代苯甲酰溴在乙醇中反应,得到相应的6-酰基-3-[(4-取代苯甲酰基)甲基]-2(3H)-苯并恶唑酮。对这些化合物进行了镇痛、抗炎活性筛选。合成的8种化合物显示出高镇痛活性,进一步研究表明化合物3、6和7是角叉菜胶和花生四烯酸诱导的爪肿胀的有效抑制剂。在用化合物3、6和7处理的小鼠中,从角叉菜胶爪肿胀液中分离出的前列腺素E2也显著降低。