SYNTHESIS OF CONFORMATIONALLY RESTRICTED SUBSTANCE-P ANTAGONISTS

被引：12
|
作者：
HOWARD, HR
SHENK, KD
COFFMAN, KC
BRYCE, DK
CRAWFORD, RT
MCLEAN, SA
机构：
[1] Central Research Division, Pfizer Inc, Groton
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1995年 / 5卷 / 02期
基金：
美国国家卫生研究院;
关键词：
D O I：
10.1016/0960-894X(94)00467-T
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Reaction of CP-99,994 (1) with benzyl chloromethyl ether under basic conditions produced the novel 1,6-diazabicyclo[3.2.1]octane system in good yield; analogs containing this nucleus display high binding affinity for substance P receptors. The ethylene homologue of 1a, diamine 7, shows enhanced inhibitory activity and may more closely approximate the binding conformation of la at the NK1 receptor.
引用
收藏
页码：111 / 114
页数：4
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