Nonpeptide glycoprotein IIb/IIIa inhibitors. 13. design and synthesis of an orally active pyrazolopiperazinone nonpeptide fibrinogen receptor antagonist

The synthesis and antiplatelet activity of a series of pyrazolopiperazinone nonpeptide fibrinogen receptor antagonists is reported. The sulfonamide analog 6 (L-734, 115), significantly inhibited ex vivo platelet aggregation 24 h after oral administration at doses of 1.0 and 2.0 mg/kg to dogs and rhe...

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Published in:Bioorganic & medicinal chemistry letters 1997-06, Vol.7 (12), p.1531-1536
Main Authors: Askew, B.C., McIntyre, C.J., Hunt, C.A., Claremon, D.A., Baldwin, J.J., Anderson, P.S., Gould, R.J., Lynch, R.J., Chang, C.C-T., Cook, J.J., Lynch, J.J., Holahan, M.A., Sitko, G.R., Stranieri, M.T.
Format: Article
Language:English
Subjects:
Biological and medical sciences
Blood. Blood coagulation. Reticuloendothelial system
Medical sciences
Pharmacology. Drug treatments
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Summary:The synthesis and antiplatelet activity of a series of pyrazolopiperazinone nonpeptide fibrinogen receptor antagonists is reported. The sulfonamide analog 6 (L-734, 115), significantly inhibited ex vivo platelet aggregation 24 h after oral administration at doses of 1.0 and 2.0 mg/kg to dogs and rhesus monkeys, respectively. The synthesis and antiplatelet activity of a series of pyrazolopiperazinone nonpeptide fibrinogen receptor antagonists is reported. The sulfonamide analog 6 (L-734,115), significantly inhibited ex vivo platelet aggregation 24 h after oral administration at doses of 1.0 and 2.0 mg/kg to dogs and rhesus monkeys, respectively.
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(97)00256-4