Synthesis of 2-[[(4-Fluoroalkoxy-2-pyridyl)methyl]sulfinyl]-1H-benzimidazoles as Antiulcer Agents

Keiji KUBO; Katsuaki ODA; Tatsuhiko KANEKO; Hioroshi SATOH; Akira NOHARA

doi:10.1248/cpb.38.2853

Keiji KUBO, Katsuaki ODA, Tatsuhiko KANEKO, Hioroshi SATOH, Akira NOHARA

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Keywords: 2-[[(4-fluoroalkoxy-2-pyridyl)methyl]sulfinyl]-1H benzimidazole, 2-[[[3-methyl-4-(2, 2, 2-trifluoroethoxy)-2-pyridyl]methyl]sulfinyl]-1H-benzimidazole, AG-1749, lansoprazole, antisecretory activity, antiulcer activity, cytoprotective activity, (H⁺+K⁺)-ATPase inhibitor

JOURNAL FREE ACCESS

1990 Volume 38 Issue 10 Pages 2853-2858

DOI https://doi.org/10.1248/cpb.38.2853

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Abstract

Many 2-[[(4-fluoroalkoxy-2-pyridyl)methyl]sulfinyl]-1H-benzimidazoles were synthesized and tested for antisecretory, antiulcer, and cytoprotective activities. Most of these compounds were superior to omeprazole in antisecretory and antiulcer potencies, and especially in protecting the gastric mucosa from ethanol-induced damage. Among these compounds 2-[[[3-methyl-4-(2, 2, 2-trifluoroethoxy)-2-pyridyl]methyl]sulfinyl]-1H-benzimidazole, AG-1749 (lansoprazole) (6f), was selected for further development and clinical evaluation.

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