Antiulcer Agents. II. Synthesis and Gastric Acid Antisecretory Activity of N-[3-{3-(Piperidinomethyl)phenoxy}propyl]-4-(1-methyl-1H-tetrazol-5-ylthio)butanamide and Related Compounds

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概要

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• N-[3-{3-(Piperidinomethyl)phenoxy}propyl]butanamides having a 1-methyl-1H-tetrazol-5-ylthio moiety as a pharmacophore and related compounds were prepared and tested for their antisecretory activity against histamine-induced gastric acid secretion in conscious rats with gastric fistulas. Most of the compounds showed antisecretory activity. Among them, N-[3-{3-(piperidinomethyl)phenoxy}propyl]-4-(1-methyl-1H-tetrazol-5-ylthio)butanamide (5f) was found to possess the most potent activity, and a possibility of isosteric replacement of the methoxycarbonyl group with 1-methyl-1H-tetrazol-5-yl group was indicated. The structure-activity relationships are also discussed.

• 社団法人日本薬学会の論文
• 1991-06-25

著者

• 植田 育男

  Institute Of Scientific And Industrial Reseach Osaka University

• 植田 育男

  The Institute of Scientific and Industrial Research, Osaka University

• 石井 克幸

  The Institute of Scientific and Industrial Research, Osaka University

• 畠中 稔

  The Institute of Scientific and Industrial Research, Osaka University

• 篠崎 勝雄

  Central Research Laboratories, Zeria Pharmaceutical Co., Ltd.

• 精木 雅雄

  Central Research Laboratories, Zeria Pharmaceutical Co., Ltd.

• 畠中 稔

  The Institute Of Scientific And Industrial Research Osaka University

• 石井 克幸

  The Institute Of Scientific And Industrial Research Osaka University

• 篠崎 勝男

  Central Research Laboratories Zeria Pharmaceutical Co. Ltd.

• 精木 雅雄

  Central Research Laboratories Zeria Pharmaceutical Co. Ltd.

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