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Design and synthesis of an orally active GPIIb/IIIa antagonist based on a phenylpiperazine scaffold.
Bioorg Med Chem Lett
; 8(12): 1531-6, 1998 Jun 16.
Article
in English
| MEDLINE
| ID: mdl-9873384
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.