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

BC Askew, CJ McIntyre, CA Hunt, DA Claremon…

Index: Askew; McIntyre; Hunt; Claremon; Baldwin; Anderson; Gould; Lynch; Chang; Cook; Holahan; Sitko; Stranieri Bioorganic and Medicinal Chemistry Letters, 1997 , vol. 7, # 12 p. 1531 - 1536

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Citation Number: 26

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.