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Design and synthesis of an orally active GPIIb/IIIa antagonist based on a phenylpiperazine scaffold
J H van Maarseveen1, J A den Hartog, K Tipker
1Solvay Pharmaceuticals Research Laboratory, Weesp, The Netherlands. jan.vanmaarseveen@solvay.com
Bioorganic & Medicinal Chemistry Letters
|January 5, 1999
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.