ANTIULCER AGENTS .1. GASTRIC ANTISECRETORY AND CYTOPROTECTIVE PROPERTIES OF SUBSTITUTED IMIDAZO[1,2-A]PYRIDINES

被引:148
作者
KAMINSKI, JJ
BRISTOL, JA
PUCHALSKI, C
LOVEY, RG
ELLIOTT, AJ
GUZIK, H
SOLOMON, DM
CONN, DJ
DOMALSKI, MS
WONG, SC
GOLD, EH
LONG, JF
CHIU, PJS
STEINBERG, M
MCPHAIL, AT
机构
[1] Pharmaceutical Research Division, Schering-Plough Corporation, Bloomfield, New Jersey
[2] Department of Chemistry, Duke University, Durham, North, Carolina
关键词
D O I
10.1021/jm00145a006
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A novel class of antiulcer agents, the substituted imidazo[1, 2-a]pyridines, is described. The present compounds are not histamine (H2) receptor antagonists nor are they prostaglandin analogues, yet they exhibit both gastric antisecretory and cytoprotective properties. The mechanism of gastric antisecretory activity may involve inhibition of the H+/K+-ATPase enzyme. Structure-activity studies led to the identification of 3-(cyanomethyl)-2-methyl-8-(phenylmethoxy)imidazo[1, 2-a] pyridine, SCH 28080 (27), which was selected for further development and clinical evaluation. © 1985, American Chemical Society. All rights reserved.
引用
收藏
页码:876 / 892
页数:17
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