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Bioorg Med Chem. 2012 Jun 15;20(12):3925-38. doi: 10.1016/j.bmc.2012.04.014. Epub 2012 Apr 14.

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

Author information

1
Pharmaceutical Research Division, Takeda Pharmaceutical Company, Ltd., 26-1, Muraokahigashi 2-chome, Fujisawa, Kanagawa 251-8555, Japan. haruyuki.nishida@takeda.com

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, compound 17c exhibited potent inhibitory action on histamine-stimulated gastric acid secretion in rats and Heidenhain pouch dogs.

PMID:
22579619
DOI:
10.1016/j.bmc.2012.04.014
[Indexed for MEDLINE]
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