Design and synthesis of novel heterobiaryl amides as metabotropic glutamate receptor subtype 5 antagonists

被引：26

作者：

Kulkarni, Santosh S. ^{[1
]}

Newman, Amy Hauck ^{[1
]}

机构：

[1] NIDA, Med Chem Sect, Intramural Res Program, NIH,DHHS, Baltimore, MD 21224 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2007年 / 17卷 / 07期

关键词：

D O I：

10.1016/j.bmcl.2006.12.083

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of heterobiaryl amides was designed and synthesized as novel mGluR5 antagonists. The synthesis using palladium catalyzed Suzuki-Miyaura cross-coupling reactions provided art array of compounds with a range of in vitro activities. In particular, compound 9e, 4( 3,5-difluorophenyl)-N-(6-methylpyridin-1-yl)picolinamide, exhibited nanomolar affinity at the mGluR5 and will serve as a template for future drug design. (c) 2007 Elsevier Ltd. All rights reserved.

引用

页码：2074 / 2079

页数：6

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