1,3-Diaminopropan-2-ol Sulfonamides as potent and selective inhibitors of the glycine transporter type 1

被引：10
|
作者：
Rahman, Shahzad S. [1 ]
Coulton, Steven
Herdon, Hugh J.
Joiner, Graham F.
Jin, Jian
Porter, Roderick A.
机构：
[1] GlaxoSmithKline Inc, Harlow CM19 5AW, Essex, England
[2] GlaxoSmithKline Inc, Collegeville, PA 19426 USA
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2007年 / 17卷 / 06期
关键词：
GlyT-1; schizophrenia; NMDA; transporter; 1,3-diaminopropan-2-ol;
D O I：
10.1016/j.bmcl.2006.12.063
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
High throughput screening led to the discovery of a novel series of 1,3-diaminopropan-2-ol sulfonarnides as selective GlyT-1 inhibitors. Structure-activity relationships of this novel series and optimisation of the initial hit that led to the identification of (2), a potent and selective GlyT-1 inhibitor, are also presented. (c) 2007 Elsevier Ltd. All rights reserved.
引用
收藏
页码：1741 / 1745
页数：5
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