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. 2003 Apr 17;13(8):1463-7.
doi: 10.1016/s0960-894x(03)00168-9.

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

Otmar Klingler  1 , Hans Matter, Manfred Schudok, S Paul Bajaj, Joerg Czech, Martin Lorenz, Hans Peter Nestler, Herman Schreuder, Peter Wildgoose
Affiliations

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

Otmar Klingler et al. Bioorg Med Chem Lett. .

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.

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