N6-substituted C5′-modified adenosines as A1 adenosine receptor agonists

被引：18

作者：

Ashton, T. D. ^{[1
]}

Baker, Stephen P. ^{[2
]}

Hutchinson, Sally A. ^{[3
]}

Scammells, Peter J. ^{[1
]}

机构：

[1] Monash Univ, Victorian Coll Pharm, Dept Med Chem, Parkville, Vic 3052, Australia

[2] Univ Florida, Coll Med, Dept Pharmacol & Therapeut, Gainesville, FL 32610 USA

[3] CSIRO Text & Fibre Technol, Belmont, Vic 3216, Australia

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2008年 / 16卷 / 04期

基金：

澳大利亚研究理事会;

关键词：

adenosine; A(1)AR agonist;

D O I：

10.1016/j.bmc.2007.11.010

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：

Adenosines bearing 5'-modification in conjunction with an N-6-substituent have previously been shown to act as partial agonists at the A(1) adenosine receptor. Our current work investigates the effect of modifying the 5'-position in conjunction with efficacious bicyclic and tricyclic N-6-substituents. Several highly potent agonists for the A(1) adenosine receptor were identified; however, all of these compounds behaved as full agonists. In keeping with previous reports, 5'-halogen and 5'-sulfide derivatives of N-6-(endo-norborn-2-yl) adenosine were, in general, low nanomolar agonists of the A(1) adenosine receptor. The known partial agonist, N-6-cyclopentyl-5'-deoxy-5'-ethylthioadenosine (2), also behaved as a full agonist in our assay. (C) 2007 Elsevier Ltd. All rights reserved.

引用

页码：1861 / 1873

页数：13

共 23 条

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