Synthesis and Gastroprokinetic Activity of 2-Amino-N-[(4-benzyl-2-morpholinyl) methyl] benzamide Derivatives

  • KATO Shiro
    Exploratory Research Laboratories, Dainippon Pharmaceutical Co., Ltd.
  • MORIE Toshiya
    Exploratory Research Laboratories, Dainippon Pharmaceutical Co., Ltd.
  • OHNO Kazunori
    Exploratory Research Laboratories, Dainippon Pharmaceutical Co., Ltd.
  • YOSHIDA Naoyuki
    Exploratory Research Laboratories, Dainippon Pharmaceutical Co., Ltd.
  • YOSHIDA Toyokichi
    Exploratory Research Laboratories, Dainippon Pharmaceutical Co., Ltd.
  • NARUTO Shunsuke
    Exploratory Research Laboratories, Dainippon Pharmaceutical Co., Ltd.

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Description

2-Alkoxy-4-amino-N-[(4-benzyl-2-morpholinyl)methyl]-5-chlorobenzamides had been identified as the interesting members of a series of selective and potent gastroprokinetic agents. A new series of 2-amino- and 2-(substituted amino)-N-[(4-benzyl-2-morpholinyl)methyl]benzamides (13-35) has been synthesized and these compounds were examined to determine whether they have advantages over the 2-morpholinyl benzamides 1 with a 2-alkoxy group.The gastroprokinetic activity was generally reduced, but several compounds showed relatively potent activity, comparable to that of the standard agent, metoclopramide. N-[(4-Benzyl-2-morpholinyl)methyl]-4-chloro-2-[(4-chlorobenzoyl)amino]benzamide (32) showed the most potent activity in this series.

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Details 詳細情報について

  • CRID
    1570291227417369984
  • NII Article ID
    110003631521
  • NII Book ID
    AA00602100
  • ISSN
    00092363
  • Text Lang
    en
  • Data Source
    • CiNii Articles

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