Syntheses of 2-(3,4-Dimethoxyphenyl)ethylamine Derivatives and Their Antiulcer Activities

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概要

• 論文の詳細を見る

• A series of acyl derivatives of 2-(3,4-dimethoxyphenyl)ethylamine (4) were synthesized and evaluated for their effectiveness to prevent water-immersion stress-induced gastric ulceration when given intraperitoneally to rats. Among them N-[2-(3,4-dimethoxyphenyl)ethyl]-2-phenylaminoacetamide hydrochloride (15) had significant antiulcer activity. Further modification of the four parts of 15 revealed that only the introduction of a carbamoyl group into 2- or 3-position of the phenylamino part gave compounds (49-51,54 and 55) which retained antiulcer activity comparable to the lead compound. However, the compounds (49-51 and 54) did not exert a prophylactic effect when administered orally except for the 3-substituted bezamide derivative 55. Alkyl substitution on the nitrogen of benzamide gave 3-[[[2-(3,4-dimethoxyphenyl)ethyl]carbamoyl]methyl]amino-N-methylbenzamide (66,DQ-2511) and the related compounds (67,70,74 and 77) which all had potent antiuler activities at oral doses of 50-400 mg/kg.

• 社団法人日本薬学会の論文
• 1992-10-25

著者

• 浅野 昌英

  第一製薬株式会社 (東京研究開発センター) 医薬開発第一部

• 細上 徹

  Exploratory Research Laboratories III, Daiichi Pharmaceutical Co., Ltd.,

• 東 邦彦

  Exploratory Research Laboratories Iii Daiichi Pharmaceutical Co. Ltd.

• 榑谷 昌彦

  Exploratory Research Laboratories III, Daiichi Pharmaceutical Co., Ltd.,

• 浅野 昌英

  Exploratory Research Laboratories III, Daiichi Pharmaceutical Co., Ltd.,

• 大屋 和美

  Exploratory Research Laboratories III, Daiichi Pharmaceutical Co., Ltd.,

• 高杉 紀雄

  Exploratory Research Laboratories III, Daiichi Pharmaceutical Co., Ltd.,

• 真船 英一

  Exploratory Research Laboratories III, Daiichi Pharmaceutical Co., Ltd.,

• 三木 藤作

  Exploratory Research Laboratories III, Daiichi Pharmaceutical Co., Ltd.,

• 細上 徹

  第一製薬株式会社 (東京研究開発センター) 探索第三研究所

• 細上 徹

  Exploratory Research Laboratories Iii Daiichi Pharmaceutical Co. Ltd.

• 三木 藤作

  Exploratory Research Laboratories Iii Daiichi Pharmaceutical Co. Ltd.

• 真船 英一

  第一製薬(株)開発研究所

• 高杉 紀雄

  第一製薬(株)開発研究所

• 細上 徹

  New Product Research Laboratories Iii Daiichi Pharmaceutical Co. Ltd.

• Takasugi Norio

  Drug Delivery Research Center Developmental Research Laboratories Daiichi Pharmaceutical Co. Ltd.

• 榑谷 昌彦

  Exploratory Research Laboratories Iii Daiichi Pharmaceutical Co. Ltd.

• 大屋 和美

  Developmental Research Laboratories, Daiichi Pharmaceutical Co., Ltd.,

• 大屋 和美

  Developmental Research Laboratories Daiichi Pharmaceutical Co. Ltd.

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