Rational design, synthesis, and structure-activity relationship of benzoxazolones: New potent mglu5 receptor antagonists based on the fenobam structure

被引：26
|
作者：
Ceccarelli, Siniona M. [1 ]
Jaeschke, Georg
Buettelmann, Bernd
Huwyler, Joerg
Kolczewski, Sabine
Peters, Jens-Uwe
Prinssen, Eric
Porter, Richard
Spooren, Will
Vieira, Eric
机构：
[1] F Hoffmann La Roche & Co Ltd, Div Pharmaceut, Discovery Res, CH-4070 Basel, Switzerland
[2] Univ Appl Sci, Northwestern Switzerland Inst Pharma Technol, CH-4132 Muttenz, Switzerland
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2007年 / 17卷 / 05期
关键词：
mGluR5; fenobam; anxiety; MPEP; benzoxazolone;
D O I：
10.1016/j.bmcl.2006.12.006
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A novel class of potent and stable mGlu5 receptor antagonists was developed by combining information from a high-throughput screening campaign with the structure of the known anxiolytic fenobam. Representative compounds from this class show favorable pharmacokinetic properties and are active in an in vivo model of anxiety. (c) 2006 Elsevier Ltd. All rights reserved.
引用
收藏
页码：1302 / 1306
页数：5
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