Synthesis of 2-amino-5-benzoyl-4-(2-furyl)thiazoles as adenosine A2A receptor antagonists

被引：26

作者：

Cole, Andrew G. ^{[1
]}

Stauffer, Tara M. ^{[1
]}

Rokosz, Laura L. ^{[1
]}

Metzger, Axel ^{[1
]}

Dillard, Lawrence W. ^{[1
]}

Zeng, Wenguang ^{[1
]}

Henderson, Ian ^{[1
]}

机构：

[1] Pharmacopeia Inc, Princeton, NJ 08543 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2009年 / 19卷 / 02期

关键词：

Adenosine; GPCR; Aminothiazole; Parkinson's disease; Combinatorial chemistry; ECLiPS (TM); L-DOPA; CAFFEINE;

D O I：

10.1016/j.bmcl.2008.11.066

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The discovery and synthesis of a series of 2-amino-5-benzoyl-4-(2-furyl)thiazoles as adenosine A(2A) receptor antagonists from a small-molecule combinatorial library using a high-throughput radioligand-binding assay is described. Antagonists were further characterized in the A(2A) binding assay and an A(1) selectivity assay. Selected examples exhibited excellent affinity for A(2A) and good selectivity versus the A(1) receptor. (C) 2008 Elsevier Ltd. All rights reserved.

引用

页码：378 / 381

页数：4

共 28 条

[21] Adenosine A2A receptor antagonists improve deficits in initiation of movement and sensory motor integration in the unilateral 6-hydroxydopamine rat model of Parkinson's disease [J].