Discovery of novel hydroxy pyrazole based factor IXa inhibitor

Synthesis and biological data of a novel selective and efficacious factor IXa inhibitor are described along with its crystal structure in factor VIIa.

Replacement of central phenol in 1 with hydroxy pyrazole resulted in compound 2 which selectively inhibits factor IXa. It is also selective against trypsin-like serine proteases in the coagulation cascade.Figure optionsDownload as PowerPoint slide