Carba-nucleosides as potent antagonists of the adenosine 5′-diphosphate (ADP) purinergic receptor (P2Y12) on human platelets

被引:9
|
作者
Ye, Hong [1 ]
Chen, Cailin [1 ]
Zhang, Han-Cheng [1 ]
Haertlein, Barbara [1 ]
Parry, Tom J. [1 ]
Damiano, Bruce P. [1 ]
Maryanoff, Bruce E. [1 ]
机构
[1] Johnson & Johnson Pharmaceut Res & Dev, Spring House, PA 19477 USA
关键词
ADP receptor; antagonist; nucleosides; P2Y(12) receptor; platelet; purinergic;
D O I
10.1002/cmdc.200700310
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
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 P2Y12 antagonists. Some tetrazole derivatives were high-affinity receptor antagonists and potent inhibitors of human platelet aggregation. (Chemical Equation Presented) © 2008 Wiley-VCH Verlag GmbH & Co. KGaA.
引用
收藏
页码:732 / 736
页数:5
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