Synthesis, Gastrointestinal Prokinetic Activity and Structure-Activity Relationships of Novel N-[[2-(Dialkylamino)ethoxy)benzyl]benzamide Derivatives

Jun SAKAGUCHI; Hiroyuki NISHINO; Nobuo OGAWA; Yuji IWANAGA; Shingo YASUDA; Hideo KATO; Yasuo ITO

doi:10.1248/cpb.40.202

Jun SAKAGUCHI, Hiroyuki NISHINO, Nobuo OGAWA, Yuji IWANAGA, Shingo YASUDA, Hideo KATO, Yasuo ITO

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Keywords: N-[[2-(dialkylamino)ethoxy]benzyl]benzamide, antiemetic activity, gastrointestinal prokinetic activity, acetylcholinesterase inhibition, structure-activity relationship

JOURNAL FREE ACCESS

1992 Volume 40 Issue 1 Pages 202-211

DOI https://doi.org/10.1248/cpb.40.202

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Abstract

Nobel N-[[2-(dialkylamino)ethoxy]benzyl]benzamide derivatives (II-1-51), derived form the structural modification of metoclopramide (i), were synthesized and examined for their pharmacological activities. Among them, N-[4-[2-(dimethylamino)ethoxy]benzyl]-3, 4-dimethoxybenzamide (II-34) which exhibited well balanced gastrointestinal prokinetic and antiemetic activities was selected as a new type of gastrointestinal prokinetic agent.

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