Nonpeptide Glycoprotein Iib/Iiia Inhibitors .13. Design And Synthesis Of An Orally Active Pyrazolopiperazinone Nonpeptide Fibrinogen Receptor Antagonist.

B.C. Askew,C.J. McIntyre,C.A. Hunt,D.A. Claremon,J.J. Baldwin,P.S. Anderson,R.J. Gould,R.J. Lynch,C.C-T. Chang,J.J. Cook,J.J. Lynch,M.A. Holahan,G.R. Sitko,M.T. Stranieri

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS（1997）

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Abstract

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. (C) 1997 Elsevier Science Ltd.

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Key words

glycoprotein

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