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Design and synthesis of an orally active GPIIb/IIIa antagonist based on a phenylpiperazine scaffold. 1998
J H van Maarseveen, and
J A den Hartog, and
K Tipker, and
J H Reinders, and
J Brakkee, and
U Schön, and
W Kehrbach, and
C G Kruse
Solvay Pharmaceuticals Research Laboratory, Weesp, The Netherlands. jan.vanmaarseveen@solvay.com
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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Thrombosis research,
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Journal of medicinal chemistry,
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Blood coagulation & fibrinolysis : an international journal in haemostasis and thrombosis,
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March 2001,
Chemical & pharmaceutical bulletin,
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J H Reinders, and
J Brakkee, and
U Schön, and
W Kehrbach, and
C G Kruse
January 2001,
Cardiovascular drug reviews,
