Carba‐nucleosides as Potent Antagonists of the Adenosine 5′‐Diphosphate (ADP) Purinergic Receptor (P2Y₁₂) on Human Platelets

Abstract

Antagonizing a key platelet purinergic receptor. The wide clinical use of clopidogrel has highlighted the importance of platelet ADP receptor (P2Y12) antagonists for preventing adverse cardiovascular events. We synthesized a series of novel carba-nucleosides and examined their usefulness as P2Y12 antagonists. Some tetrazole derivatives were high-affinity receptor antagonists and potent inhibitors of human platelet aggregation.