SYNTHESIS AND ANTIULCER ACTIVITY OF N-SUBSTITUTED N'-[3-[3-(PIPERIDINOMETHYL)PHENOXY]PROPYL]UREAS - HISTAMINE-H2-RECEPTOR ANTAGONISTS WITH A POTENT MUCOSAL PROTECTIVE ACTIVITY

被引：18
|
作者：
MIYASHITA, M
MATSUMOTO, T
MATSUKUBO, H
IINUMA, F
TAGA, F
SEKIGUCHI, H
HAMADA, K
OKAMURA, K
NISHINO, K
机构：
[1] CENT RES LAB,2399-1 MITARAI,NOGI,TOCHIGI 32901,JAPAN
[2] KYORIN PHARMACEUT CO LTD,TECH CTR ORGAN SYNTH,OKAYA 394,JAPAN
来源：
JOURNAL OF MEDICINAL CHEMISTRY | 1992年 / 35卷 / 13期
关键词：
D O I：
10.1021/jm00091a012
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
As an aim toward developing new antiulcer agents, new N-substituted N'-[3-[3-(piperidinomethyl)phenoxylpropyl]ureas were synthesized and evaluated for histamine H-2-receptor antagonistic, gastric antisecretory, and gastric mucosal protective activities. A QSAR study showed that the most favorable N-substituents were electron-donating straight-chain alkyl groups of short length such as ethyl group from the viewpoint of dual action, i.e., gastric antisecretory and mucosal protective actions. Among the ureas studied, compounds 4, 5, and 8-10 were selected as candidates for further study.
引用
收藏
页码：2446 / 2451
页数：6
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