Bioorganic and Medicinal Chemistry Letters p. 1531 - 1536 (1998)
Update date:2022-08-04
Topics: Selectivity Clinical Trials Lead Optimization Regulatory Approval Toxicity and Safety Assessment Toxicity and Safety Formulation Functional Group Introduction Lipophilicity and Solubility Metabolic Stability Bioisosteric Replacement
Van Maarseveen, Jan H.
Den Hartog, Jack A.J.
Tipker, Koos
Reinders, Jan-Hendrik
Brakkee, Joost
Schoen, Uwe
Kehrbach, Wolfgang
Kruse, Chris G.
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.
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