Design and synthesis of an orally active GPIIb/IIIa antagonist based on a phenylpiperazine scaffold

Article abstract of DOI:10.1016/S0960-894X(98)00257-1

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.