Title of article :
Design, synthesis, and structure–activity relationship of a new class of amidinophenylurea-based factor VIIa inhibitors
Author/Authors :
Otmar Klingler، نويسنده , , Hans Matter، نويسنده , , Manfred Schudok، نويسنده , , S. Paul Bajaj، نويسنده , , Joerg Czech، نويسنده , , Martin Lorenz، نويسنده , , Hans Peter Nestler، نويسنده , , Herman Schreuder، نويسنده , , Peter Wildgoose، نويسنده ,
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.
