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
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.
引用
收藏
页码:523 / 526
页数:4
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