Biphenyl-indanones: Allosteric potentiators of the metabotropic glutamate subtype 2 receptor

被引：43

作者：

Bonnefous, C

Vernier, JM

Hutchinson, JH

Gardner, MF

Cramer, M

James, JK

Rowe, BA

Daggett, LP

Schaffhauser, H

Kamenecka, TM

机构：

[1] Merck Res Labs, Dept Med Chem, San Diego, CA 92121 USA

[2] Merck Res Labs, Dept Neuropharmacol, San Diego, CA 92121 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2005年 / 15卷 / 19期

关键词：

mGluR2; indanone; CNS; schizophrenia;

D O I：

10.1016/j.bmcl.2005.06.062

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

We have identified and synthesized a series of biphenyl-carboxylic acid indanones as allosteric potentiators of the metabotropic glutamate receptor 2. Structure-activity relationship studies directed toward improving the potency and the brain to plasma ratio of the initial lead led to the discovery of 5 and 23 (EC50 = 111 and 5 nM, respectively). (c) 2005 Elsevier Ltd. All rights reserved.

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收藏

页码：4354 / 4358

页数：5

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