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

被引:26
|
作者
Askew, BC [1 ]
McIntyre, CJ [1 ]
Hunt, CA [1 ]
Claremon, DA [1 ]
Baldwin, JJ [1 ]
Anderson, PS [1 ]
Gould, RJ [1 ]
Lynch, RJ [1 ]
Chang, CCT [1 ]
Cook, JJ [1 ]
Lynch, JJ [1 ]
Holahan, MA [1 ]
Sitko, GR [1 ]
Stranieri, MT [1 ]
机构
[1] MERCK RES LABS,DEPT PHARMACOL,W POINT,PA 19486
关键词
D O I
10.1016/S0960-894X(97)00256-4
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
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.
引用
收藏
页码:1531 / 1536
页数:6
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