Reversible inhibitors of the gastric (H+/K+)-ATPase. 2. 1-Arylpyrrolo [3, 2-c] quinolines: effect of the 4-substituent

CA Leach, TH Brown, RJ Ife, DJ Keeling…

Index: Leach, Colin A.; Brown, Thomas H.; Ife, Robert J.; Keeling, David J.; Laing, Shiona M.; et al. Journal of Medicinal Chemistry, 1992 , vol. 35, # 10 p. 1845 - 1852

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Citation Number: 57

Abstract

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 ...