- Discovery of a novel, orally active himbacine-based thrombin receptor antagonist (SCH 530348) with potent antiplatelet activity.
Discovery of a novel, orally active himbacine-based thrombin receptor antagonist (SCH 530348) with potent antiplatelet activity.
Journal of medicinal chemistry (2008-05-02)
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, Madhu Chintala
PMID18447380
ABSTRACT
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.
MATERIALS