The discovery of SCH 530348 provides a novel, orally active PAR-1 antagonist with potent antiplatelet activity for potential use in acute coronary syndrome.
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.
Chackalamannil et al. (2008) studied this question.