2-Aminothiophene-3-carboxylates and carboxamides as adenosine A1 receptor allosteric enhancers

被引：81
作者：
Nikolakopoulos, G
Figler, H
Linden, J
Scammells, PJ
机构：
[1] Monash Univ, Victorian Coll Pharm, Dept Med Chem, Parkville, Vic 3052, Australia
[2] Univ Virginia, Dept Med Cardiol, Charlottesville, VA 22908 USA
[3] Univ Virginia, Dept Pharmacol, Charlottesville, VA 22908 USA
来源：
BIOORGANIC & MEDICINAL CHEMISTRY | 2006年 / 14卷 / 07期
关键词：
adenosine; allosteric enhancer; adenosine A(1) receptor;
D O I：
10.1016/j.bmc.2005.11.018
中图分类号：
Q5 [生物化学]; Q7 [分子生物学];
学科分类号：
071010 ; 081704 ;
摘要：
Three series of 2-amino-4,5,6,7-tetrahydrobenzo[b]thiophene and 2-amino-5,6,7,8-tetrahydrocyclohepta[b]thiophenes with 3-carboxylates and carboxamides have been prepared using the Gewald synthesis and evaluated as AIAR allosteric enhancers. The structure-activity relationships of these classes of compound are described. A number of compounds, notably 7b, are more potent and efficacious than PD81,723 (1). (c) 2005 Elsevier Ltd. All rights reserved.
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收藏
页码：2358 / 2365
页数：8
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