Allosteric potentiators of the metabotropic glutamate receptor 2 (mGlu2). Part 1: Identification and synthesis of phenyl-tetrazolyl acetophenones

被引：30

作者：

Pinkerton, AB ^{[1
]}

Cube, RV ^{[1
]}

Hutchinson, JH ^{[1
]}

Rowe, BA ^{[1
]}

Schaffhauser, H ^{[1
]}

Zhao, XM ^{[1
]}

Daggett, LP ^{[1
]}

Vernier, JM ^{[1
]}

机构：

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

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2004年 / 14卷 / 21期

关键词：

metabotropic glutamate receptors; GPCRs;

D O I：

10.1016/j.bmcl.2004.08.020

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 aryl-tetrazoyl acetophenones as positive allosteric potentiators of the metabotropic glutamate receptor 2. Structure activity relationship studies directed toward improving the potency and level of potentiation led to the discovery of 22 (EC50 = 93 nM, 128% potentiation). (C) 2004 Elsevier Ltd. All rights reserved.

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页码：5329 / 5332

页数：4

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