Studies on Antiulcer Drugs. III. Synthesis and Antiulcer Activities of Imidazo(1,2-a)pyridinylethylbenzoxazoles and Related Compounds. A Novel Class of Histamine H2-Receptor Antagonists.
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A series of imidazo[1, 2-a]pyridinylalkylbenzoxazole derivatives was synthesized and tested for histamine H<SUB>2</SUB>-receptor antagonist, gastric antisecretory and antiulcer activities. Some of 2-amino-6-[2-(imidazo[1, 2-a]pyridin-2-yl)ethyl]benzoxazole derivatives were found to have good pharmacological activities. Among them, 2-amino-6-[2-(7-methoxy-3-methylimidazo[1, 2-a]pyridin-2-yl)ethyl]benzoxazole (II-11) and 2-acetamido-6-[2-(7-methylimidazo[1, 2-a]pyridin-2-yl)ethyl]benzoxazole (II-38) showed potent antisecretory and cytoprotective activity. The structure-activity relationships of these compounds are discussed.
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社団法人 日本薬学会 | 論文
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