Antagonists of the human A2A receptor. Part 5: Highly bio-available pyrimidine-4-carboxamides

被引：25
|
作者：
Gillespie, Roger J. [2 ]
Bamford, Samantha J. [2 ]
Gaur, Suneel [2 ]
Jordan, Allan M. [1 ]
Lerpiniere, Joanne [2 ]
Mansell, Howard L. [2 ]
Stratton, Gemma C. [2 ]
机构：
[1] Vernalis R D Ltd, Cambridge CB21 6GB, England
[2] Vernalis R D Ltd, Winnersh Wokingham RG41 5UA, England
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2009年 / 19卷 / 10期
关键词：
Adenosine receptor; Parkinson's disease; Pyrimidine; Carboxamide; PARKINSONS-DISEASE; L-DOPA; ADENOSINE; DESIGN; DERIVATIVES; DYSKINESIA; AGONISTS; KW-6002; MONKEYS; POTENT;
D O I：
10.1016/j.bmcl.2009.03.142
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A novel series of antagonists of the human A(2A) receptor have been identified and have been shown to display good potency and high degrees of selectivity over other receptor sub-types. Displaying in vivo potency in commonly used disease models and high oral bio-availability, this class of compounds may serve as clinically useful treatments for the relief of the symptoms associated with Parkinson's disease. (C) 2009 Elsevier Ltd. All rights reserved.
引用
收藏
页码：2664 / 2667
页数：4
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