Discovery and SAR of 6-substituted-4-anilinoquinazolines as non-competitive antagonists of mGlu5

被引：20

作者：

Felts, Andrew S. ^{[1
,3
]}

Saleh, Sam A. ^{[1
,3
]}

Le, Uyen ^{[1
,3
]}

Rodriguez, Alice L. ^{[1
,3
]}

Weaver, C. David ^{[1
,3
]}

Conn, P. Jeffrey ^{[1
,3
]}

Lindsley, Craig W. ^{[1
,2
,3
]}

Emmitte, Kyle A. ^{[1
,3
]}

机构：

[1] Vanderbilt Univ, Med Ctr, Dept Pharmacol, Nashville, TN 37232 USA

[2] Vanderbilt Univ, Dept Chem, Nashville, TN 37232 USA

[3] Vanderbilt Inst Chem Biol, Vanderbilt Program Drug Discovery, Nashville, TN 37232 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2009年 / 19卷 / 23期

关键词：

Glutamate; Metabotropic glutamate receptor 5; Negative allosteric modulator; Non-competitive antagonist; Quinazoline; METABOTROPIC GLUTAMATE-RECEPTOR-5; ALLOSTERIC MODULATORS; RECEPTOR ANTAGONISTS; MGLUR5; ANTAGONISTS; POTENT; MTEP; PHARMACOLOGY; SUPPRESSION; INHIBITORS; LY456236;

D O I：

10.1016/j.bmcl.2009.10.024

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A high-throughput cell-based screen identified a series of 6-substituted-4-anilinoquinazolines as noncompetitive antagonists of metabotropic glutamate receptor 5 (mGlu(5)). This Letter describes the SAR of this series and the profile of selected compounds in selectivity and radioligand binding assays. (C) 2009 Elsevier Ltd. All rights reserved.

引用

页码：6623 / 6626

页数：4

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