Aix-Marseille Université, Institut des Sciences Moléculaires de Marseille, iSm2-UMR CNRS 6263, Centre Saint Jérôme, Service 532, 13397, Marseille Cedex 20, France.
Org Biomol Chem. 2010 Sep 7;8(17):3874-81. doi: 10.1039/c0ob00017e. Epub 2010 Jul 9.
The synthesis of new C-6 1,2,3-triazole adenosine derivatives via microwave assisted 1,3-dipolar cycloaddition as key step is described. The binding on membranes of cells that over express A(1) adenosine receptors (A(1)AR) was also evaluated. Among them, four compounds increased cAMP production, in a dose-dependent manner acting as antagonists of the A(1)AR, while two compounds act as agonists.
本文描述了通过微波辅助 1,3-偶极环加成反应作为关键步骤合成新型 C-6 1,2,3-三唑腺苷衍生物。还评估了它们与过度表达 A(1)腺苷受体（A(1)AR）的细胞膜的结合。其中，有 4 种化合物以剂量依赖的方式增加 cAMP 的产生，作为 A(1)AR 的拮抗剂，而另外 2 种化合物则作为激动剂。
