5-Amidinobenzo [b] thiophenes as dual inhibitors of factors IXa and Xa

…, X Cheng, DP Modi, KA Rossi, JM Luettgen…

文献索引：Qiao, Jennifer X.; Cheng, Xuhong; Modi, Dilip P.; Rossi, Karen A.; Luettgen, Joseph M.; Knabb, Robert M.; Jadhav, Prabhakar K.; Wexler, Ruth R. Bioorganic and Medicinal Chemistry Letters, 2005 , vol. 15, # 1 p. 29 - 35

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被引用次数: 52

摘要

... The hydrophobic interaction of the benzothiophene ring with the wall of the S1 pocket and the polarizable and sterically larger sulfur atom appear to be favorable in improving selectivity relative to fXa. Table 1. Compound, X, Y, R′ (+/−, fIXa K i , μM, fXa K i , μM, fIXa/fXa, Trypsin K i , μM, Thrombin K i , μM. 1, 0.66, 0.00063, 1048, 0.15, 0.60. ... 20, NH, F, CH 2 Ph, 0.063, 0.0025, 25, 0.34, 13. 21, S, H, CH 2 Ph-p-NH 2, 0.074, 0.047, 1.6, >4.2, 4.2. ...