Doğruer D S, Unlü S, Sahin M F, Yeşilada E
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Gazi University, Ankara, Turkey.
Farmaco. 1998 Jan;53(1):80-4. doi: 10.1016/s0014-827x(97)00017-7.
Sixteen (2-benzothiazolone-3-yl and 2-benzoxazolone-3-yl) acetic acid derivatives 5 have been tested for anti-nociceptive and anti-inflammatory activity in this study, 4-[2-(6-Benzoyl-2-benzoxazolone-3-yl)acetyl]morpholine (5c), 4-¿2-[6-(2-chloro-benzoyl)-2-benzoxazolone-3-yl]acetyl¿morpholine (5d), 1-[2-(5-chloro-2-benzoxazolone-3-yl)acetyl]pyrrolidine (5f), methyl (6-methyl-2-benzoxazolone-3-yl)acetate (5k) and N,N-diethyl-2-(2-benzothiazolone-3-yl)acetamide (5m) have shown more potent anti-nociceptive activity than others. Among these compounds, 5c, 5d and 5m have exhibited good anti-inflammatory activity, with 5f, and to a lesser extent, the other molecules displaying some toxic potential.
本研究对16种（2-苯并噻唑啉-3-基和2-苯并恶唑啉-3-基）乙酸衍生物5进行了抗伤害感受和抗炎活性测试，4-[2-(6-苯甲酰基-2-苯并恶唑啉-3-基)乙酰基]吗啉（5c）、4-[2-[6-(2-氯苯甲酰基)-2-苯并恶唑啉-3-基]乙酰基]吗啉（5d）、1-[2-(5-氯-2-苯并恶唑啉-3-基)乙酰基]吡咯烷（5f）、(6-甲基-2-苯并恶唑啉-3-基)乙酸甲酯（5k）和N,N-二乙基-2-(2-苯并噻唑啉-3-基)乙酰胺（5m）显示出比其他化合物更强的抗伤害感受活性。在这些化合物中，5c、5d和5m表现出良好的抗炎活性，5f以及其他分子在较小程度上显示出一定的毒性潜力。
