State Key Laboratory of Chemical Resource Engingeering, Department of Organic Chemistry, College of Science, Beijing University of Chemical Technology, Beijing 100029, China.
Eur J Med Chem. 2012 Jul;53:114-23. doi: 10.1016/j.ejmech.2012.03.047. Epub 2012 Apr 4.
A series of novel N(6)-alkyl(aryl)-2-alkyl(aryl)thioadenosines were synthesized, and their human antiplatelet aggregation activities were evaluated by the stimulation of adenosine 5'-diphosphate (ADP). Some of these compounds showed strong activity, among which compound 5b(11) displayed the highest activity with an IC(50) value of 29 ± 3 μM. Furthermore, five compounds were tested against arachidonic acid (AA)-induced human platelet aggregation. The results showed that compound 5b(10) exhibited the highest activity with an IC(50) value of 3 ± 2 μM. The adenosine derivatives substituted with a phenethyl group at the N(6) position and a methylthio or ethylthio group at the C-2 position displayed high antiplatelet aggregation activity.
合成了一系列新型 N(6)-烷（芳）基-2-烷（芳）基硫代腺苷，并通过 5'-二磷酸腺苷（ADP）的刺激评估了它们对人血小板聚集的抑制活性。其中一些化合物表现出很强的活性，其中化合物 5b(11)表现出最高的活性，IC(50)值为 29±3μM。此外，还对 5 种化合物进行了花生四烯酸（AA）诱导的人血小板聚集的测试。结果表明，化合物 5b(10)表现出最高的活性，IC(50)值为 3±2μM。在 N(6)位取代苯乙基和 C-2 位取代甲基硫代或乙基硫代的腺苷衍生物具有很高的抗血小板聚集活性。
