Synthesis of 2-[[(4-fluoroalkoxy-2-pyridyl)methyl]sulfinyl]-1H- benzimidazoles as antiulcer agents |
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Authors: | K Kubo K Oda T Kaneko H Satoh A Nohara |
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Affiliation: | Research and Development Division, Takeda Chemical Industries, Ltd., Osaka, Japan. |
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Abstract: | Many 2-[[(4-fluoroalkoxy-2-pyridyl)methyl]sulfinyl]-1H-benzimidazoles were synthesized and tested for anti-secretory, antiulcer, and cytoprotective activities. Most of these compounds were superior to omeprazole in anti-secretory 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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