Himbacine derived thrombin receptor antagonists: discovery of a new tricyclic core.

Himbacine derived thrombin receptor antagonists: discovery of a new tricyclic core.

Bioorganic & medicinal chemistry letters (2007-05-11)

Martin C Clasby, Samuel Chackalamannil, Michael Czarniecki, Darío Doller, Keith Eagen, William J Greenlee, Yan Lin, Jayaram R Tagat, Hsingan Tsai, Yan Xia, Ho-Sam Ahn, Jacqueline Agans-Fantuzzi, George Boykow, Madhu Chintala, Yunsheng Hsieh, Andrew T McPhail

PMID17490877

摘要

The synthesis and biological activity of a novel series of thrombin receptor antagonists is described. This series of compounds showed excellent in vitro and in vivo potency. The most potent compound 40 had an IC(50) of 7.6 nM and showed robust inhibition of platelet aggregation in a cynomolgus monkey model after oral administration.