5-aminomethylquinoxaline-2,3-diones, Part III: Arylamide derivatives as highly potent and selective glycine-site NMDA receptor antagonists

被引：24

作者：

Acklin, P ^{[1
]}

Allgeier, H ^{[1
]}

Auberson, YP ^{[1
]}

Bischoff, S ^{[1
]}

Ofner, S ^{[1
]}

Sauer, D ^{[1
]}

Schmutz, M ^{[1
]}

机构：

[1] Novartis Pharma AG, CH-4002 Basel, Switzerland

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1998年 / 8卷 / 05期

关键词：

D O I：

10.1016/S0960-894X(98)00055-9

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of quinoxaline-2,3-diones with very high affinity to the glycine site of the NMDA receptor has been discovered. In contrast to the 7-nitro derivatives, the most potent 7-bromo substituted compounds were highly selective for the glycine site. Although none of the described compounds were active in the electroshock model in mice, la displayed significant protection in the quinolinic acid-induced excitotoxicity model in vivo. (C) 1998 Elsevier Science Ltd. All rights reserved.

引用

页码：493 / 498

页数：6

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