Synthesis and SAR comparison of regioisomeric aryl naphthyridines as potent mGlu5 receptor antagonists

被引：25

作者：

Galatsis, Paul ^{[1
]}

Yamagata, Koji ^{[1
]}

Wendt, John A. ^{[1
]}

Connolly, Cleo J. ^{[1
]}

Mickelson, John W. ^{[1
]}

Milbank, Jared B. J. ^{[1
]}

Bove, Susan E. ^{[2
,3
]}

Knauer, Christopher S. ^{[2
,3
]}

Brooker, Rachel M. ^{[2
,3
]}

Augelli-Szafran, Corinne E. ^{[1
]}

Schwarz, Roy D. ^{[2
,3
]}

Kinsora, Jack J. ^{[2
,3
]}

Kilgore, Kenneth S. ^{[2
,3
]}

机构：

[1] Pfizer Global REs & Dev, Dept Med Chem, Ann Arbor, MI 48105 USA

[2] Pfizer Global REs & Dev, Dept CNS Biol, Ann Arbor, MI 48105 USA

[3] Pfizer Global REs & Dev, Dept Inflammat, Ann Arbor, MI 48105 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2007年 / 17卷 / 23期

关键词：

mGlu5; receptor; antagonist; 1,5-naphthyridine; 1,6-naphthyridine; 1,8-naphthyridine; rat; osteoarthritis; pain;

D O I：

10.1016/j.bmcl.2007.09.083

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

We describe three novel regioisomeric series of aryl naphthyridine analogs, which are potent antagonists of the Class III GPCR mGlu5 receptor. The synthesis and in vitro and in vivo pharmacological activities of these analogs are discussed. (c) 2007 Elsevier Ltd. All rights reserved.

引用

页码：6525 / 6528

页数：4

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