Studies on Proton Pump Inhibitors. II. : Synthesis and Antiulcer Activity of 8-[(2-Benzimidazolyl)-sulfinylmethyl]-1,2,3,4-tetrahydroquinolines and Related Compounds

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概要

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• Many 8-[(2-benzimidazolyl)sulfinylmethyl]-1,2,3,4-tetrahydroquinoline derivatives were synthesized and tested for their (H^+ + K^+)adenosine triphosphatase (ATPase)-inhibitory and antisecretory activities against histamine-induced gastric acid secretion in rats. These sulfinyl compounds were synthesized by the oxidation of the corresponding sulfides, which were obtained from the reaction of 8-chloromethyl-1,2,3,4-tetrahydroquinolines and 2-mercaptobenzimidazoles in the presence of potassium carbonate. All compounds tested were potent inhibitors of (H^+ + K^+)ATPase. Most of the compounds showed antisecretory activity. Among them, 8-[(2-benzimidazolyl)sulfinylmethyl]-1-ethyl-1,2,3,4-tetrahydroquinoline (IXa) was found to have the most potent activity. The structure-activity relationships are discussed.

• 社団法人日本薬学会の論文
• 1989-08-25

著者

• 山崎 勝也

  大阪市立大学医学部生体情報解析学講座

• 山下 博司

  Tokushima Research Institute Otsuka Pharmaceutical Co. Ltd.

• 中川 量之

  2nd Tokushima Institute Of New Drugs Research Otsuka Pharmaceutical Co. Ltd.

• 中川 量之

  大塚製薬株式会社有機化学研究所

• 中川 量之

  Tokushima Research Institute Otsuka Pharmaceutical Co. Ltd.

• 中川 量之

  大塚製薬株式会社徳島研究所

• 藪内 洋一

  Tokushima Research Institute, Otsuka Pharmaceutical Co., Ltd.,

• 藪内 洋一

  Tokushima Research Institute Otsuka Pharmaceutical Co. Ltd.

• 藪内 洋一

  大塚製薬徳島研究所

• Yamasaki K

  Faculty Of Pharmaceutical Sciences Teikyo Heisei University

• 内多 稔

  Tokushima Research Institute, Otsuka Pharmaceutical Co., Ltd.,

• 森田 清司

  Tokushima Research Institute, Otsuka Pharmaceutical Co., Ltd.,

• 神辺 敏実

  Tokushima Research Institute, Otsuka Pharmaceutical Co., Ltd.,

• 山崎 勝也

  Tokushima Research Institute, Otsuka Pharmaceutical Co., Ltd.,

• 千尋 正利

  Tokushima Research Institute, Otsuka Pharmaceutical Co., Ltd.,

• Morita S

  Tokushima Research Institute Otsuka Pharmaceutical Co. Ltd.

• Uchida Masaki

  Faculty Of Pharmaceutical Sciences Josai University

• Yamasaki K

  Division Of Medicinal Chemistry Graduate School Of Biomedical Sciences Hiroshima University

• 千壽 正利

  Tokushima Research Institute Otsuka Pharmaceutical Co. Ltd.

• Uchida Masaatsu

  Departments Of Pharmacology Meiji Pharmaceutical University

• 神辺 敏実

  Tokushima Research Institute Otsuka Pharmaceutical Co. Ltd.

• Uchida Mihoko

  Department Of Biochemistry Faculty Of Pharmaceutical Sciences Hoshi University

• Morita S

  Kagawa Medical Univ. Kagawa Jpn

• Uchida M

  Otsuka Pharmaceutical Co. Ltd. Tokushima Jpn

• Morita Shushi

  Department Of Hospital Pharmacy Kagawa University

• 森田 清司

  Tokushima Research Institute Otsuka Pharmaceutical Co. Ltd.

• 千尋 正利

  Tokushima Research Institute Otsuka Pharmaceutical Co. Ltd.

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