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

页码：1741 / 1745

页数：5

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