Discovery of a novel, orally active himbacine-based thrombin receptor antagonist (SCH 530348) with potent antiplatelet activity.

@article{Chackalamannil2008DiscoveryOA,
  title={Discovery of a novel, orally active himbacine-based thrombin receptor antagonist (SCH 530348) with potent antiplatelet activity.},
  author={Samuel Chackalamannil and Yuguang Wang and William J. Greenlee and Zhiyong Hu and Yan Xia and H S Ahn and George C Boykow and Yunsheng Hsieh and Jairam R. Palamanda and Jacqueline Agans-Fantuzzi and Stan Kurowski and Michael J. Graziano and Madhu S. Chintala},
  journal={Journal of medicinal chemistry},
  year={2008},
  volume={51 11},
  pages={
          3061-4
        }
}
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. 

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