Discovery of N-(2-aryl-cyclohexyl) substituted spiropiperidines as a novel class of GlyT1 inhibitors

被引：23

作者：

Pinard, E ^{[1
]}

Ceccarelli, SM ^{[1
]}

Stalder, H ^{[1
]}

Alberati, D ^{[1
]}

机构：

[1] F Hoffmann La Roche & Co Ltd, Pharmaceut Res, Discovery Chem, CH-4070 Basel, Switzerland

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2006年 / 16卷 / 02期

关键词：

GlyT1; GlyT2; NMDA; schizophrenia; transporter; glycine; spiropiperidine;

D O I：

10.1016/j.bmcl.2005.09.075

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Screening of the Roche compound library led to the identification of cis-N-(2-phenyt-cyclohexyl)-spiropiperidine 1 as structurally novel GlyT1 inhibitor. The SAR, which was developed in this series, resulted in the discovery of highly potent compounds displaying excellent selectivity against the GlyT2 isoform. (c) 2005 Elsevier Ltd. All rights reserved.

引用

页码：349 / 353

页数：5

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