Synthesis, anti-platelet aggregation activity evaluation and structure-activity relationships of a series of novel purine derivatives

摘要

This article described how further extensive variation of the substituents on the purine scaffold of adenosine triphosphate (ATP), and the human anti-platelet aggregation activities were modified in order to find exploitation of the structure-activity relationships (SAR). A series of novel designed 6-alkylamino-2-alkylthio-9-hydroxyalkyl(carbalkoxy) purine derivatives were synthesized via a modification procedure, and the human anti-platelet aggregation activities were evaluated. The SAR of these compounds were analyzed in detail, and the results of the structural requirements of the substituents to improve potency may provide a basis for the development of potent P2Y(12) antagonists.