2-styryl-pyridines and 2-(3,4-dihydro-naphthalen-2-yl)-pyridines as potent NR1/2B subtype selective NMDA receptor antagonists

被引：4

作者：

Buettelmann, B ^{[1
]}

Alanine, A

Bourson, A

Gill, R

Heitz, MP

Mutel, V

Pinard, E

Trube, G

Wyler, R

机构：

[1] F Hoffmann La Roche Ltd, Div Pharma, Discovery Chem, CH-4070 Basel, Switzerland

[2] F Hoffmann La Roche Ltd, Div Pharma, Preclin CNS Res, CH-4070 Basel, Switzerland

来源：

CHIMIA | 2004年 / 58卷 / 09期

关键词：

neurodegeneration; NMDA; NR1/2B antagonists; structure-activity relationship;

D O I：

10.2533/000942904777677579

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

A series of 2-styryl-pyridines and 2-(3,4-dihydro-naphthalen-2-yl)-pyridines was prepared and evaluated as NR1/2B subtype selective NMDA receptor antagonists. The SAR developed in this series resulted in the discovery of high affinity antagonists that are selective (vs. alpha(1) and M-1 receptors) and are active in vivo.

引用

页码：630 / 633

页数：4