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

页码：2664 / 2667

页数：4

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