Muto Y, Ichikawa H, Seiki M, Shirataki Y, Yokoe I, Komatsu M
Central Research Laboratories, Zeria Pharmaceutical Co., Ltd., Saitama, Japan.
Yakugaku Zasshi. 1995 Apr;115(4):307-17. doi: 10.1248/yakushi1947.115.4_307.
It was found that (+/-)ethyl 2-[2-(3-hydroxypropyl)-4-oxocyclohexylidene]-propionate (1), (+/-)ethyl 2-[2-(3-hydroxypropyl)-4,5-dimethoxyphenyl]propionate (2) and (+/-)3-[2-(3-hydroxypropyl)-4,5-dimethoxyphenyl]-2-butanone (3) had excellent antiulcer activities. In order to study structure-activity relationships, (+/-)2-[(3-hydroxypropyl)phenyl]cyclopentanone derivatives (4, 5) and (+/-)2-[(3-hydroxypropyl)phenyl]cyclopentanol derivatives (6, 7) were synthesized and tested for antiulcer activities. As a result, (+/-)2-[2-(3-hydroxypropyl)-4-methoxy-5-(2- piperidinoethoxy)phenyl]cyclopentanone (5k) exhibited potent antiulcer activities.
已发现（±）2-[2-(3-羟丙基)-4-氧代环己叉基]丙酸乙酯（1）、（±）2-[2-(3-羟丙基)-4,5-二甲氧基苯基]丙酸乙酯（2）和（±）3-[2-(3-羟丙基)-4,5-二甲氧基苯基]-2-丁酮（3）具有优异的抗溃疡活性。为了研究构效关系，合成了（±）2-[(3-羟丙基)苯基]环戊酮衍生物（4, 5）和（±）2-[(3-羟丙基)苯基]环戊醇衍生物（6, 7）并测试其抗溃疡活性。结果，（±）2-[2-(3-羟丙基)-4-甲氧基-5-(2-哌啶基乙氧基)苯基]环戊酮（5k）表现出强效抗溃疡活性。
