Structure-activity relationships of N-substituted 4-(trifluoromethoxy) benzamidines with affinity for GluN2B-containing NMDA receptors

被引：20

作者：

Beinat, Corinne ^{[1
]}

Banister, Samuel D. ^{[1
,2
]}

Hoban, Jane ^{[1
]}

Tsanaktsidis, John ^{[3
]}

Metaxas, Athanasios ^{[4
]}

Windhorst, Albert D. ^{[4
]}

Kassiou, Michael ^{[1
,2
,5
]}

机构：

[1] Univ Sydney, Sch Chem, Sydney, NSW 2006, Australia

[2] Brain & Mind Res Inst, Sydney, NSW 2050, Australia

[3] CSIRO Mat Sci & Engn, Ian Wark Lab, Clayton, Vic 3168, Australia

[4] Vrije Univ Amsterdam, Med Ctr, Dept Radiol & Nucl Med, NL-1081 HV Amsterdam, Netherlands

[5] Univ Sydney, Discipline Med Radiat Sci, Sydney, NSW 2006, Australia

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2014年 / 24卷 / 03期

关键词：

GluN2B; NMDA; Amidine; CNS; Structure-activity relationships; ANTAGONISTS;

D O I：

10.1016/j.bmcl.2013.12.087

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

GluN2B subtype-selective NMDA antagonists represent promising therapeutic targets for the symptomatic treatment of multiple CNS pathologies. A series of N-benzyl substituted benzamidines were synthesised and the benzyl ring was further replaced with various polycyclic moieties. Compounds were evaluated for activity at GluN2B containing NMDA receptors where analogues 9, 12, 16 and 18 were the most potent of the series, replacement of the benzyl ring with polycycles resulted in a complete loss of activity. (C) 2013 Elsevier Ltd. All rights reserved.

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收藏

页码：828 / 830

页数：3

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