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Design, synthesis, and biological evaluation of potent and selective amidino bicyclic factor Xa inhibitors

…, KA Rossi, RS Alexander, AM Smallwood…

文献索引:Han; Dominguez; Stouten; Park; Duffy; Galemmo Jr.; Rossi; Alexander; Smallwood; Wong; Wright; Luettgen; Knabb; Wexler Journal of Medicinal Chemistry, 2000 , vol. 43, # 23 p. 4398 - 4415

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被引用次数: 44

摘要

Thrombotic diseases are a major cause of death and morbidity. Factor Xa (fXa) plays a vital role in the regulation of normal homeostasis and abnormal intravascular thrombus development in the blood coagulation cascade. A novel series of fXa inhibitors incorporating an amidino 6, 5-fused bicyclic moiety at the P1 position has been designed and synthesized based on molecular modeling studies. Structure-activity relationship (SAR) studies have ...