Journal of Medicinal Chemistry p. 2446 - 2451 (1992)
Update date:2022-08-05
Topics:
Miyashita
Matsumoto
Matsukubo
Iinuma
Taga
Sekiguchi
Hamada
Okamura
Nishino
As an aim toward developing new antiulcer agents, new N-substituted N'-[3- [3-(piperidinomethyl)phenoxy]propyl]ureas were synthesized and evaluated for histamine H2-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.
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