2008•ChemMedChemRequires access
Carba‐nucleosides as Potent Antagonists of the Adenosine 5′‐Diphosphate (ADP) Purinergic Receptor (P2Y12) on Human Platelets
Ye Hong, Cailin Chen, Han‐Cheng Zhang, Barbara J. Haertlein, Tom J. Parry, Bruce P. Damiano, Bruce E. Maryanoff
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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.