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Design, synthesis, and structure-activity relationship of a new class of amidinophenylurea-based factor VIIa
Otmar Klingler1, Hans Matter, Manfred Schudok
1Aventis Pharma Deutschland GmbH, Building G878, D-65926 Frankfurt, Germany. otmar.klingler@aventis.com
Bioorganic & Medicinal Chemistry Letters
|April 2, 2003
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.