Abstract
A series of novel N6-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 5b11 displayed the highest activity with an IC50 value of 29±3μM. Furthermore, five compounds were tested against arachidonic acid (AA)-induced human platelet aggregation. The results showed that compound 5b10 exhibited the highest activity with an IC50 value of 3±2μM. The adenosine derivatives substituted with a phenethyl group at the N6 position and a methylthio or ethylthio group at the C-2 position displayed high antiplatelet aggregation activity.
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