含生物电子等排体异恶唑的新型腺苷 A3 选择性配体的合成。
The synthesis of new adenosine A3 selective ligands containing bioisosteric isoxazoles.
作者信息
Mogensen J P, Roberts S M, Bowler A N, Thomsen C, Knutsen L J
机构信息
Novo Nordisk A/S, Måløv, Denmark.
出版信息
Bioorg Med Chem Lett. 1998 Jul 7;8(13):1767-70. doi: 10.1016/s0960-894x(98)00302-3.
PMID:9873431
Abstract
The synthesis and purinergic receptor binding of novel adenosine A3 ligands is described. Many selective A3 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 A3 receptor.
摘要
本文描述了新型腺苷A3配体的合成及其嘌呤能受体结合情况。许多选择性A3受体激动剂，如N-(3-碘苄基)腺苷-5'-甲基脲酰胺(IB-MECA)，都含有一个4'-核糖基烷基酰胺部分。我们发现，该酰胺及其他4'-官能团可用等排体异恶唑取代，且目标分子对重组人A3受体仍保持强效结合力。
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