Design, synthesis, and structure-activity relationship of a new class of amidinophenylurea-based factor VIIa inhibitors.

Basic Information

ID: ALA1144973

Journal: Bioorg Med Chem Lett

Title: Design, synthesis, and structure-activity relationship of a new class of amidinophenylurea-based factor VIIa inhibitors.

Authors: Klingler O, Matter H, Schudok M, Bajaj SP, Czech J, Lorenz M, Nestler HP, Schreuder H, Wildgoose P.

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 K(i) value of 23 nM for factor VIIa.

CiteXplore: 12668013

DOI: 10.1016/s0960-894x(03)00168-9

Patent ID: