Novel Benzamides as Selective and Potent Gastrokinetic Agents. IV. Synthesis and Structure-Activity Relationships of 2-Substituted 4-Amino-N-[(4-benzyl-2-morpholinyl)methyl]-5-chlorobenzamides

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概要

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• A new series of 2-substituted 4-amino-N-[(4-benzyl-2-morpholinyl)methyl]-5-chlorobenzamides (4-39) including a few 4-fluorobenzyl analogues were prepared and evaluated for their gastrokinetic activity by determining their effects on the gastric emptying activity of phenol red semisolid meal in rats. The C-2 substituent comprises alkoxy and variously substituted alkoxy groups. Among the derivatives, 4-amino-N-[(4-benzyl-2-morpholinyl)methyl]-2-(n-butoxy)-5-chlorobenzamide (5), its 4-fluorobenzyl (6), and 3-methyl-2-butenyloxy analogues (22) were superior to cisapride and essentially equipotent to the 2-ethoxy analogue (1b, AS-4370 as its citrate) in gastrokinetic activity. These compounds, like AS-4370,had no dopamine D_2 receptor antagonistic activity.

• 社団法人日本薬学会の論文
• 1992-06-25

著者

• 森江 俊哉

  Exploratory Research Laboratories, Dainippon Pharmaceutical Co., Ltd.,

• 吉田 直之

  Exploratory Research Laboratories, Dainippon Pharmaceutical Co., Ltd.,

• 賀登 志朗

  Exploratory Research Laboratories, Dainippon Pharmaceutical Co., Ltd.,

• 松本 純一

  Exploratory Research Laboratories, Dainippon Pharmaceutical Co., Ltd.,

• 森江 俊哉

  大日本製薬株式会社創薬研究所

• 松本 純一

  Exploratory Research Laboratories Dainippon Pharmaceutical Company Ltd.

• 吉田 直之

  大日本製薬(株)薬理研究所

• Kato Satoru

  Kanazawa Univ. Kanazawa Jpn

• Matsumoto J

  Discovery Research Laboratories Ii Dainippon Pharmaceutical Company Ltd.

• 賀登 志朗

  大日本製薬株式会社創薬研究所

• Yoshida Naoko

  Institute For Medical And Dental Engineering Tokyo Medical And Dental University

• Kato S

  Discovery Research Laboratories I Dainippon Pharmaceutical Co. Ltd.

• Kato S

  Chemistry Research Laboratories Dainippon Pharmaceutical Co. Ltd.

• 吉田 直之

  大日本製薬株式会社創薬研究所第一薬理研究部

• Yoshida Naotoshi

  Medicinal Plant Garden Faculty Of Pharmaceutical Sciences Hokkaido University

• 吉田 直之

  大日本製薬株式会社創薬研究所

• 松本 純一

  Exploratory Research Laboratories Dainippon Pharmaceutical Co. Ltd.

• Kato Satoru

  Department Of Molecular Neurobiology Graduate School Of Medicine University Of Kanazawa

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