Potent direct inhibitors of factor Xa based on the tetrahydroisoquinoline scaffold

RA Al-Horani, AY Mehta, UR Desai

文献索引：Al-Horani, Rami A.; Mehta, Akul Y.; Desai, Umesh R. European Journal of Medicinal Chemistry, 2012 , vol. 54, p. 771 - 783

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被引用次数: 12

摘要

Direct inhibition of coagulation factor Xa (FXa) carries significant promise for developing effective and safe anticoagulants. Although a large number of FXa inhibitors have been studied, each can be classified as either possessing a highly flexible or a rigid core scaffold. We reasoned that an intermediate level of flexibility will provide high selectivity for FXa considering that its active site is less constrained in comparison to thrombin and more ...