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新型N-[[2-(二烷基氨基)乙氧基]苄基]苯甲酰胺衍生物的合成、胃肠道促动力活性及构效关系

Synthesis, gastrointestinal prokinetic activity and structure-activity relationships of novel N-[[2-(dialkylamino)ethoxy]benzyl]benzamide derivatives.

作者信息

Sakaguchi J, Nishino H, Ogawa N, Iwanaga Y, Yasuda S, Kato H, Ito Y

机构信息

Central Research Laboratories, Hokuriku Seiyaku Co., Ltd., Fukui, Japan.

出版信息

Chem Pharm Bull (Tokyo). 1992 Jan;40(1):202-11. doi: 10.1248/cpb.40.202.

DOI:10.1248/cpb.40.202
PMID:1576675
Abstract

Novel N-[[dialkylamino)ethoxy]benzyl]benzamide derivatives (II-1-51), derived from 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.

摘要

通过对胃复安（I）进行结构修饰得到了新型N-[[二烷基氨基）乙氧基]苄基]苯甲酰胺衍生物（II-1-51），并对其药理活性进行了研究。其中，具有良好平衡的胃肠促动力和止吐活性的N-[4-[2-（二甲基氨基）乙氧基]苄基]-3,4-二甲氧基苯甲酰胺（II-34）被选为新型胃肠促动力剂。

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