Synthesis and Structure-Activity Relationship sof N-Substituted 2-[(2-Imidazolylsulfinyl)methyl]anilines as a New Class of Gastric H^+/K^+-ATPase Inhibitors
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概要
- 論文の詳細を見る
A series of N-substituted 2-[(2-imidazolylsulfinyl)methyl]anilines (3) was synthesized and evaluated for its biological activity against gastric H^+/K^+-ATPase prepared from rabbit stomach and gastric acid secretions in Heidenhain pouch dogs. Monoalkyl substituents on the nitrogen atom of the aniline moiety markedly inhibited the enzyme acticity to the same degree as omeprazole, a representative H^+/K^+-ATPase inhibitor. Most of these compounds, administered at 3 mg/kg i.v. inhibited histamine-stimulated gastric acid secretion. The inhibitory activity of these derivatives on the enzymes at pH 6.0 was more potent than that at pH 7.4,and was distinctly correlated to stability in aqueous solution at pH 5.0.
- 公益社団法人日本薬学会の論文
- 1991-07-25
著者
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岡部 進
Department Of Applied Pharmacology Kyoto Pharmaceutical University
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野村 豊
Department Of Applied Chemistry Faculty Of Engineering Saitama University
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井形 英樹
Department Of Applied Pharmacology Kyoto Pharmaceutical University
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真崎 光夫
Research Laboratories, Nippon Chemiphar Co., Ltd.,
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山川 富雄
Department Of Biochemistry Faculty Of Pharmacy Tokyo University Of Pharmacy & Life Science
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山川 富雄
Research Laboratories Nippon Chemiphar Co. Ltd.
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山川 富雄
Resarch Laboratories, Nippon Chemiphar Co., Ltd.,
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松倉 均
Resarch Laboratories, Nippon Chemiphar Co., Ltd.,
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野村 豊
Resarch Laboratories, Nippon Chemiphar Co., Ltd.,
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吉岡 満子
Resarch Laboratories, Nippon Chemiphar Co., Ltd.,
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真崎 光夫
Resarch Laboratories, Nippon Chemiphar Co., Ltd.,
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Nomura Y
Faculty Of Pharmaceutical Sciences The University Of Tokyo
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松倉 均
Resarch Laboratories Nippon Chemiphar Co. Ltd.
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吉岡 満子
Resarch Laboratories Nippon Chemiphar Co. Ltd.
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真崎 光夫
Research Laboratories Nippon Chemiphar Co. Ltd.
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