Author/Authors :
Jan H. van Maarseveen، نويسنده , , Jack A. J. den Hartog، نويسنده , , Koos Tipker، نويسنده , , Jan-Hendrik Reinders، نويسنده , , Joost Brakkee، نويسنده , , Uwe Sch?n، نويسنده , , Wolfgang Kehrbach، نويسنده , , Chris G. Kruse، نويسنده ,
Abstract :
The design and synthesis of an orally active LMW non-peptide GPIIb/IIIa antagonist, based on a N,N′-bisphenylpiperazine scaffold, is described. The optimal compound showed a high in vitro binding potency (pIC50=8.7) in combination with potent oral antithrombotic activity (30–40% inhibition of thrombus growth at 0.3–3 mg/kg) with a duration of action of >90 min. in a hamster cheek pouch model.
