Generation of potent coagulation protease inhibitors utilizing zinc-mediated chelation
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- 作者：Wendy B. Young ; Paul Sprengeler ; William D. Shrader ; Yong Li ; Roopa Rai ; Erik Verner ; Thomas Jenkins ; Paul Fatheree ; Aleksandr Kolesnikov ; James W. Janc et al.
- 关键词：Factor Xa ; Factor VIIa ; Thrombin ; Coagulation ; Protease inhibitor ; Zinc chelation
- 刊名：Bioorganic and Medicinal Chemistry Letters
- 出版年：2006
- 出版时间：1 February 2006
- 年：2006
- 卷：16
- 期：3
- 页码：710-713
- 全文大小：158 K
文摘
Inhibition of coagulation proteases such as thrombin, fXa, and fVIIa has been a focus of ongoing research to produce safe and effective antithrombotic agents. Herein, we describe a unique zinc-mediated chelation strategy to streamline the discovery of potent inhibitors of fIIa, fXa, and fVIIa. SAR studies that led to the development of selective inhibitors of fXa will also be detailed.