Development of a novel tricyclic class of potent and selective FIXa inhibitors
Review articleOpen access
2015/11/15 Short communication DOI: 10.1016/j.bmcl.2015.07.078
Journal: Bioorganic & Medicinal Chemistry Letters
AbstractUsing structure based drug design, a novel class of potent coagulation factor IXa (FIXa) inhibitors was designed and synthesized. High selectivity over FXa inhibition was achieved. Selected compounds were evaluated in rat IV/PO pharmacokinetic (PK) studies and demonstrated desirable oral PK profiles. Finally, the pharmacodynamics (PD) of this class of molecules were evaluated in thrombin generation assay (TGA) in Corn Trypsin Inhibitor (CTI) citrated human plasma and demonstrated characteristics of a FIXa inhibitor.
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