SYNTHESIS OF 2-[[(4-FLUOROALKOXY-2-PYRIDYL)METHYL]SULFINYL]-1H-BENZIMIDAZOLES AS ANTIULCER AGENTS

被引：60
|
作者：
KUBO, K [1 ]
ODA, K [1 ]
KANEKO, T [1 ]
SATOH, H [1 ]
NOHARA, A [1 ]
机构：
[1] TAKEDA CHEM IND LTD, DIV RES & DEV, 2-17-85 JUSOHONMACHI, YODOGAWA KU, OSAKA 532, JAPAN
来源：
CHEMICAL & PHARMACEUTICAL BULLETIN | 1990年 / 38卷 / 10期
关键词：
2,2-trifluoroethoxy)-2-pyridyl]methyl]sulfinyl]-lH-benzimidazole AG-1749 lansoprazole antisecretory activity antiulcer activity cytoprotective activity (H+ + K +)-ATPase inhibitor; 2-[[(4-fluoroalkoxy-2-pyridyl)methyl]sulfinyl]-1 H-benzimidazole 2-[[[3-methyl-4-(2;
D O I：
10.1248/cpb.38.2853
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Many 2-[[(4-fluoroalkoxy-2-pyridyl)methyl]sulfinyl]-lH-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-trifiuoroethoxy)-2-pyridyl]methyl]sulfinyl]-lH-benzimidazole, AG-1749 (lansoprazole) (6f), was selected for further development and clinical evaluation. © 1990, The Pharmaceutical Society of Japan. All rights reserved.
引用
收藏
页码：2853 / 2858
页数：6
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