REVERSIBLE INHIBITORS OF THE GASTRIC (H+/K+)-ATPASE .2. 1-ARYLPYRROLO[3,2-C]QUINOLINES - EFFECT OF THE 4-SUBSTITUENT

被引：58

作者：

LEACH, CA

BROWN, TH

IFE, RJ

KEELING, DJ

LAING, SM

PARSONS, ME

PRICE, CA

WIGGALL, KJ

机构：

[1] SmithKline Beecham Pharmaceuticals R & D, Herts AL6 9AR, Frythe, Welwyn

[2] AB Hässle, S-431 83, Mölndal

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 1992年 / 35卷 / 10期

关键词：

D O I：

10.1021/jm00088a021

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Further work on compounds 1 has identified the 4-position as a site where substantial modifications are tolerated, leading to analogues which are more potent and less toxic than those described previously. The best compound in the series is 13a (SK&F 96356), which is a potent inhibitor of gastric acid secretion in both the pentagastrin-stimulated rat and the histamine-stimulated dog. This compound shows reversible, K+-competitive binding to the enzyme. Because of its fluorescent properties, it is also proving useful in vitro as a probe of the structure and function of the (H+/K+)-ATPase.

引用

页码：1845 / 1852

页数：8