Pyrrolylquinoxalinediones: A new class of AMPA receptor antagonists

被引：19

作者：

Lubisch, W ^{[1
]}

Behl, B ^{[1
]}

Hofmann, HP ^{[1
]}

机构：

[1] KNOLL AG,DEPT CNS PHARMACOL,D-67008 LUDWIGSHAFEN,GERMANY

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1996年 / 6卷 / 23期

关键词：

D O I：

10.1016/S0960-894X(96)00534-3

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Pyrrolylquinoxalinediones were synthesized and their affinities for the AMPA receptor were determined. Most compounds showed moderate to good affinities. The acetic acid derivative 8b exhibited a K-i value of 70 nM and was equipotent to NBQX 1. Structure activity relationships are discussed. Selected compounds were tested for their potency to inhibit AMPA induced lethal convulsions in mice. In this in vivo model the compounds showed improved potency compared with NBQX. Copyright (C) 1996 Elsevier Science Ltd

引用

页码：2887 / 2892

页数：6

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