Allosteric potentiators if the metabotrophic glutamate receptor 2 (mGlu2). Part 2: 4-thiopyridyl acetophenones as non-tetrazole containing mGlu2 receptor potentiators

被引：23

作者：

Pinkerton, AB ^{[1
]}

Cube, RV ^{[1
]}

Hutchinson, JH ^{[1
]}

James, JK ^{[1
]}

Gardner, MF ^{[1
]}

Schaffhauser, H ^{[1
]}

Rowe, BA ^{[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 / 23期

关键词：

GPCRs; glutamate receptors; schizophrenia; allosteric;

D O I：

10.1016/j.bmcl.2004.09.028

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 4-thiopyridyl acetophenones as positive allosteric potentiators of the metabotropic glutamate receptor 2. Structure-activity relationship studies directed toward replacement of the tetrazole in the initial lead led to the discovery of 16 (EC50 = 340 nM), which showed improved brain penetration over the initial lead. (C) 2004 Elsevier Ltd. All rights reserved.

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页码：5867 / 5872

页数：6

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