Discovery of a Novel, Orally Active Himbacine-Based Thrombin Receptor Antagonist (SCH 530348) with Potent Antiplatelet Activity
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- 作者：Samuel Chackalamannil ; Yuguang Wang ; William J. Greenlee ; Zhiyong Hu ; Yan Xia ; Ho-Sam Ahn ; George Boykow ; Yunsheng Hsieh ; Jairam Palamanda ; Jacqueline Agans-Fantuzzi ; Stan Kurowski ; Michael Graziano ; M
- 刊名：Journal of Medicinal Chemistry
- 出版年：2008
- 出版时间：June 12, 2008
- 年：2008
- 卷：51
- 期：11
- 页码：3061 - 3064
- 全文大小：87K
- 年卷期：v.51,no.11(June 12, 2008)
- ISSN：1520-4804
文摘
The discovery of an exceptionally potent series of thrombin receptor (PAR-1) antagonists based on the natural product himbacine is described. Optimization of this series has led to the discovery of 4 (SCH 530348), a potent, oral antiplatelet agent that is currently undergoing Phase-III clinical trials for acute coronary syndrome (unstable angina/non-ST segment elevation myocardial infarction) and secondary prevention of cardiovascular events in high-risk patients.