Chemical and Pharmaceutical Bulletin
Online ISSN : 1347-5223
Print ISSN : 0009-2363
ISSN-L : 0009-2363
Synthesis and Gastroprokinetic Activity of 2-Amino-N-[(4-benzyl-2-morpholinyl)methyl]benzamide Derivatives
賀登 志朗森江 俊哉大野 一教吉田 直之吉田 豊吉成戸 俊介
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1995 年 43 巻 4 号 p. 582-587

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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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© The Pharmaceutical Society of Japan
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