2-aminothiazoles:: A new class of agonist allosteric enhancers of A1 adenosine receptors

被引：38

作者：

Chordia, MD

Murphree, LJ

Macdonald, TL

Linden, J

Olsson, RA

机构：

[1] Univ Virginia, Dept Chem, Charlottesville, VA 22901 USA

[2] Univ Virginia, Dept Pharmacol, Charlottesville, VA 22901 USA

[3] Univ Virginia, Dept Med Cardiol, Charlottesville, VA 22901 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2002年 / 12卷 / 12期

关键词：

D O I：

10.1016/S0960-894X(02)00236-6

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

This report describes the synthesis and structure-activity relationships of a new class of A(1) adenosine receptor agonist allosteric enhancers, 2-aminothiazolium salts. The EC50 of compounds 6a, 6b, 7, and 8 were 0.3, 4.5, 3.8, and 1.2 muM, substantially lower than that of the 'Gold Standard' 2-amino-3-benzoyl thiophene (PD 81,723), which has an EC50 of 38 muM. (C) 2002 Elsevier Science Ltd. All rights reserved.

引用

页码：1563 / 1566

页数：4

共 8 条

[1]

BRUNS RF, 1990, MOL PHARMACOL, V38, P939

[2] Structure and function of adenosine receptors and their genes [J].