Why the study?
The study evaluated variations of substituents on the purine scaffold of ATP to explore structure-activity relationships for human anti-platelet aggregation activity.
The synthesis and structure-activity relationship analysis of novel purine derivatives provides a basis for developing new potent P2Y12 antagonists for anti-platelet therapy.
New purine derivatives show anti-platelet activity in vitro; hypothesis-generating and leaves open any clinical translation.
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.
No takes yet. Share an insight, caveat, or question.
Li et al. (2020) studied this question.
Synapse has enriched 5 closely related papers on similar clinical questions. Consider them for comparative context: