The synthesis of new adenosine A3 selective ligands containing bioisosteric isoxazoles

被引：22
|
作者：
Mogensen, JP
Roberts, SM
Bowler, AN
Thomsen, C
Knutsen, LJS
机构：
[1] Novo Nordisk AS, Hlth Care Discovery, DK-2760 Malov, Denmark
[2] Univ Liverpool, Dept Chem, Liverpool L69 3BX, Merseyside, England
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1998年 / 8卷 / 13期
关键词：
D O I：
10.1016/S0960-894X(98)00302-3
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
The synthesis and purinergic receptor binding of novel adenosine A, ligands is described. Many selective A, receptor agonists e.g. N-(3-iodobenzyl)adenosine-5'-methyluronamide (IB-MECA) contain a 4'-ribosylalkylamide moiety. We found that this amide and other 4'-functional groups could be replaced with an isosteric isoxazole, and the target molecules retained potent binding to the recombinant human A, receptor. (C) 1998 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码：1767 / 1770
页数：4
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