Synthesis of 4-(phenylamino)quinoline-3-carboxamides as a Novel Class of Gastric H^+/K^+-ATPase Inhibitors

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概要

• 論文の詳細を見る

• In a search for inhibitors of gastric H^+/K^+ATPase, 4-(phenylamino)quinoline-3-carboxamides were synthesized and evaluated for antisecretory activity against histamine-induced gastric acid secretion in rats. These compounds were synthesized by condensation of aniline derivatives with N-substituted 4-chloroquinoline-3-carboxamides, which were obtained from treatment of 4(1H)-quinolinone-3-carboxylic acid with thionyl chloride. Most of the compounds inhibited histamine-induced gastric acid secretion in rats. Among them, N-allyl-4-(2-ethylphenylamino)quinoline-3-carboxamide (4h) was the most potent inhibitor and had the best profile as a candidate antiulcer agent. This compound showed reversible, K^+-competitive gastric H^+/K^+-ATPase inhibitory activity.

• 社団法人日本薬学会の論文
• 1995-04-15

著者

• 山崎 勝也

  大阪市立大学医学部生体情報解析学講座

• 松原 淳

  Tokushima Research Institute Otsuka Pharmaceutical Co. Ltd.

• 内多 稔

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

• 森田 清司

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

• 山崎 勝也

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

• 大坪 健児

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

• 大谷 直明

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

• Morita S

  Tokushima Research Institute Otsuka Pharmaceutical Co. Ltd.

• Uchida Masaki

  Faculty Of Pharmaceutical Sciences Josai University

• 大谷 直明

  Tokushima Research Institute Otsuka Pharmaceutical Co. Ltd.

• Uchida Masaatsu

  Departments Of Pharmacology Meiji Pharmaceutical University

• 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

• 大坪 健児

  Tokushima Research Institute Otsuka Pharmaceutical Co. Ltd.

• 森田 清司

  Tokushima Research Institute Otsuka Pharmaceutical Co. Ltd.

• Ohtani T

  Minase Research Institute Ono Pharmaceutical Co. Ltd.

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