CONFORMATIONALLY RESTRICTED PIPERIDINYL BENZAMIDES AS 5-HT3 RECEPTOR ANTAGONISTS

被引：5
|
作者：
BERMUDEZ, J
HADLEY, MS
KING, FD
MARTIN, RT
机构：
[1] SmithKline Beecham Pharmaceuticals, Harlow, Essex CM19 5AD, Coldharbour Road, The Pinnacles
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1992年 / 2卷 / 06期
关键词：
D O I：
10.1016/S0960-894X(01)81190-2
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
The synthesis and 5-HT3 receptor antagonist activity of indolizidin-7-yl and 8-oxaquinolizidin-2-yl benzamides related to the quinolizidine, BRL 20627 (2), are described. High potency is restricted to axial isomers and both the indolizidines and oxa-quinolizidines are much more potent than (2), an effect which appears to be unrelated to basicity.
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页码：523 / 526
页数：4
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