STRUCTURE-ACTIVITY-RELATIONSHIPS IN A SERIES OF 3-SULFONYLAMINO-2-(1H)-QUINOLONES, AS NEW AMPA KAINATE AND GLYCINE ANTAGONISTS

被引：33

作者：

CORDI, AA ^{[1
]}

DESOS, P ^{[1
]}

RANDLE, JCR ^{[1
]}

LEPAGNOL, J ^{[1
]}

机构：

[1] INST RECH SERVIER, F-92150 SURESNES, France

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 1995年 / 3卷 / 02期

关键词：

D O I：

10.1016/0968-0896(95)00007-4

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

This paper describes the design and synthesis of a new class of molecules, the 3-sulfonylamino-2-(1H)-quinolones, which are potent and selective antagonists at both the AMPA/kainate site as well as at the NMDA-associated glycine site. The molecules were characterized by their binding affinities to rat cortical membranes and by electrophysiology on Xenopus oocytes injected with mRNA isolated from rat cerebral cortex. The most potent compound 61 has an IC50 of 0.09 mu M for binding at the AMPA/kainate site, and 0.16 mu M in oocyte electrophysiology.

引用

页码：129 / 141

页数：13

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