Design, Synthesis, and Structure—Activity Relationship of a New Class of Amidinophenylurea-Based Factor VIIa Inhibitors.

Abstract Selective inhibition of coagulation factor VIIa has recently gained attraction as interesting approach towards antithrombotic treatment. Using parallel synthesis supported by structure-based design and X-ray crystallography, we were able to identify a novel series of amidinophenylurea derivatives with remarkable affinity for factor VIIa. The most potent compound displays a Ki value of 23 nM for factor VIIa.