Studies on Proton Pump Inhibitors. I. : Synthesis of 8-[(2-Benzimidazoly)sulfinyl]-5,6,7,8-tetrahydroquinolines and Related Compounds

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概要

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• Many 8-[(2-benzimidazolyl)sulfinyl]-5,6,7,8-tetrahydroquinolines were synthesized and examined for their (H^+ + K^+) adenosine triphoshatase ATPase-inhibitory and antisecretory activities. These sulfinyl compounds could be considered to be rigid analogues of the 2-[(2-pyridyl)methylsulfinyl]benzimidazole class of antisecretoey agents. All the compounds tested were potent inhibitors of (H^+ + K^+)ATPase. Most of the compounds also inhibited histamine-induced gastric acid secretion in rats. Among them, 8-[(5-fluoro-2-benzimidazoly)sulfinyl]-3-methyl-5,6,7,8-tetrahydroquinoline (XIVm) 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
• 1989-06-25

著者

• 山崎 勝也

  大阪市立大学医学部生体情報解析学講座

• 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.,

• 千壽 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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