| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1392883 | European Journal of Medicinal Chemistry | 2012 | 10 Pages |
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 ± 3 μM. 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 ± 2 μM. 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.
Graphical abstractA series of novel N6-alkyl(aryl)-2-alkyl(aryl)thioadenosines were synthesized and evaluated for their human antiplatelet activities.Figure optionsDownload full-size imageDownload as PowerPoint slideHighlights► A series of novel N6-alkyl(aryl)-2-alkyl(aryl)thioadenosines were synthesized. ► Their human antiplatelet activities were also evaluated. ► Compounds 5b10 and 5b11 showed excellent antiplatelet activity. ► The structure–activity relationships of these novel compounds have been discussed.
