Design of selective phenylglycine amide tissue factor/factor VIIa inhibitors

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• 作者：Groebke Zbinden ; Katrin ; Banner ; David W. ; Ackermann ; Jean ; D芒芒芒Arcy ; Allan ; Kirchhofer ; Daniel ; et. al.
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2005
• 期刊代码：10_0960894x
• 类别：ch
• 出版时间：February 1, 2005
• 卷：15
• 期：3
• 页码：817-822
• 文件大小：350 K

摘要

Proof of concept experiments have shown that tissue factor/factor VIIa inhibitors have antithrombotic activity without enhancing bleeding propensity. Starting from lead compounds generated by a biased combinatorial approach, phenylglycine amide tissue factor/factor VIIa inhibitors with low nanomolar affinity and good selectivity against other serine proteases of the coagulation cascade were designed, using the guidance of X-ray structural analysis and molecular modelling.