Discovery and SAR of small molecule PAR1 antagonists

High-throughput screening resulted in the identification of a small molecule inhibitor of PAR1. Optimisation of the initial hit led to the discovery of compounds 34 and 49, which displayed antithrombotic activity in an arteriovenous shunt model in the rat after iv administration.

Graphical abstractThe development of novel small molecule inhibitors of PAR1 is described.Figure optionsDownload full-size imageDownload as PowerPoint slide