Title of article
Design and Synthesis of an orally active GPIIb/IIIa antagonist based on a phenylpiperazine scaffold
Author/Authors
Jan H. van Maarseveen، نويسنده , , Jack A. J. den Hartog، نويسنده , , Koos Tipker، نويسنده , , Jan-Hendrik Reinders، نويسنده , , Joost Brakkee، نويسنده , , Uwe Sch?n، نويسنده , , Wolfgang Kehrbach، نويسنده , , Chris G. Kruse، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 1998
Pages
6
From page
1531
To page
1536
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.
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
1998
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
789466
Link To Document