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Carba‐nucleosides as Potent Antagonists of the Adenosine 5′‐Diphosphate (ADP) Purinergic Receptor (P2Y 12 ) on Human Platelets
Author(s) -
Ye Hong,
Chen Cailin,
Zhang HanCheng,
Haertlein Barbara,
Parry Tom J.,
Damiano Bruce P.,
Maryanoff Bruce E.
Publication year - 2008
Publication title -
chemmedchem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.200700310
Subject(s) - p2y12 , purinergic receptor , adenosine diphosphate , platelet , pharmacology , chemistry , receptor , adenosine , tetrazole , purinergic signalling , p2y receptor , clopidogrel , adenosine receptor , biochemistry , platelet aggregation , medicine , stereochemistry , agonist , aspirin
Antagonizing a key platelet purinergic receptor . The wide clinical use of clopidogrel has highlighted the importance of platelet ADP receptor (P2Y 12 ) antagonists for preventing adverse cardiovascular events. We synthesized a series of novel carba‐nucleosides and examined their usefulness as P2Y 12 antagonists. Some tetrazole derivatives were high‐affinity receptor antagonists and potent inhibitors of human platelet aggregation.