Arylmethoxypyridines as novel, potent and orally active mGlu5 receptor antagonists

被引：10

作者：

Büttelmann, B

Peters, JU

Ceccarelli, S

Kolczewski, S

Vieira, E

Prinssen, EP

Spooren, W

Schuler, F

Huwyler, J

Porter, RHP

Jaeschke, G

机构：

[1] F Hoffmann La Roche Ltd, Div Pharma, Discovery Chem, CH-4070 Basel, Switzerland

[2] F Hoffmann La Roche Ltd, Div Pharma, Preclin CNS Res, CH-4070 Basel, Switzerland

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2006年 / 16卷 / 07期

关键词：

mGluR5; metabotropic glutamate receptor; anxiolytic; anxiolysis;

D O I：

10.1016/j.bmcl.2005.12.088

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Optimisation of affinity, chemical stability, metabolic stability and solubility led from a chemically labile HTS hit 1 to mGlu5 receptor antagonists (24-26) with high affinity for the allosteric M PEP binding site, improved microsomal metabolic stability and anxiolytic-like activity in vivo as assessed by the Vogel conflict drinking test. (C) 2006 Elsevier Ltd. All rights reserved.

引用

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页码：1892 / 1897

页数：6

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