Discovery, synthesis, and biological evaluation of novel pyrrole derivatives as highly selective potassium-competitive acid blockers

H Nishida, A Hasuoka, Y Arikawa, O Kurasawa…

Index: Nishida, Haruyuki; Hasuoka, Atsushi; Arikawa, Yasuyoshi; Kurasawa, Osamu; Hirase, Keizo; Inatomi, Nobuhiro; Hori, Yasunobu; Sato, Fumihiko; Tarui, Naoki; Imanishi, Akio; Kondo, Mitsuyo; Takagi, Terufumi; Kajino, Masahiro Bioorganic and Medicinal Chemistry, 2012 , vol. 20, # 12 p. 3925 - 3938

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Citation Number: 24

Abstract

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 ...