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

被引：42
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.
引用
收藏
页码：4354 / 4358
页数：5
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