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.

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页码：1767 / 1770

页数：4

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