Discovery and synthesis of a novel series of quinoline-based thrombin receptor (PAR-1) antagonists

The design, synthesis, and SAR studies of a structurally novel series of highly potent thrombin receptor (PAR-1) antagonists are described. Compound 30 is a highly potent thrombin receptor antagonist (IC50 = 6.3 nM), a related compound 36 showing efficacy in a monkey ex vivo study.

The synthesis and SAR studies of a structurally novel series of highly potent thrombin receptor (PAR-1) antagonists are described.Figure optionsDownload as PowerPoint slide