1019502-05-6Relevant articles and documents
Design and synthesis of an orally active GPIIb/IIIa antagonist based on a phenylpiperazine scaffold
Van Maarseveen, Jan H.,Den Hartog, Jack A.J.,Tipker, Koos,Reinders, Jan-Hendrik,Brakkee, Joost,Schoen, Uwe,Kehrbach, Wolfgang,Kruse, Chris G.
, p. 1531 - 1536 (1998)
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.