881673-82-1Relevant articles and documents
Identification of a novel fluoropyrrole derivative as a potassium-competitive acid blocker with long duration of action
Nishida, Haruyuki,Arikawa, Yasuyoshi,Hirase, Keizo,Imaeda, Toshihiro,Inatomi, Nobuhiro,Hori, Yasunobu,Matsukawa, Jun,Fujioka, Yasushi,Hamada, Teruki,Iida, Motoo,Nishitani, Mitsuyoshi,Imanishi, Akio,Fukui, Hideo,Itoh, Fumio,Kajino, Masahiro
supporting information, p. 3298 - 3314 (2017/05/29)
With the aim to find a novel long-lasting potassium-competitive acid blocker (P-CAB) that would perfectly overcome the limitations of proton pump inhibitors (PPIs), we tried various approaches based on pyrrole derivative 1b as a lead compound. As part of
Discovery, synthesis, and biological evaluation of novel pyrrole derivatives as highly selective potassium-competitive acid blockers
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
, p. 3925 - 3938 (2012/08/14)
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.
PROTON PUMP INHIBITORS
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, (2008/06/13)
A proton pump inhibitor containing a compound represented by the formula (I) wherein X and Y are the same or different and each is a bond or a spacer having 1 to 20 carbon atoms in the main chain, R1 is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group, R2, R3 and R4 are the same or different and each is a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted thienyl group, an optionally substituted benzo[b]thienyl group, an optionally substituted furyl group, an optionally substituted pyridyl group, an optionally substituted pyrazolyl group, an optionally substituted pyrimidinyl group, an acyl group, a halogen atom, a cyano group or a nitro group, R5 and R6 are the same or different and each is a hydrogen atom or an optionally substituted hydrocarbon group, which has a superior proton pump action and shows an antiulcer activity and the like after conversion to a proton pump inhibitor in the body, or a salt thereof. or a prodrug thereof is provided.