Macrocyclic Factor XIa Inhibitors.
Bioorganic & medicinal chemistry letters(2017)
摘要
A series of macrocyclic factor XIa (FXIa) inhibitors was designed based on an analysis of the crystal structures of the acyclic phenylimidazole compounds. Further optimization using structure-based design led to inhibitors with pM affinity for FXIa, excellent selectivity against a panel of relevant serine proteases, and good potency in the activated partial thromboplastin time (aPTT) clotting assay.
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关键词
Factor Xla inhibitors,FXIa,Activated partial thromboplastin time,aPTT,Thrombosis
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