期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 20, 期 12, 页码 3925-3938出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2012.04.014
关键词
Pyrrole; H+,K+-ATPase; Potassium-competitive acid blocker
To discover a gastric antisecretory agent more potent than existing proton pump inhibitors, novel pyrrole derivatives were synthesized, and their H+, K+-ATPase inhibitory activities and inhibitory action on histamine-stimulated gastric acid secretion in rats were evaluated. Among the compounds synthesized, compound 17a exhibited selective and potent H+, K+-ATPase inhibitory activity through reversible and K+-competitive ionic binding; furthermore, compound 17c exhibited potent inhibitory action on histamine-stimulated gastric acid secretion in rats and Heidenhain pouch dogs. (C) 2012 Elsevier Ltd. All rights reserved.
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