参考标题:Synthesis Of A Homologous Series Of Ketomethylene Arginyl Pseudodipeptides And Application To Low Molecular Weight Hirudin-Like Thrombin Inhibitors 作者:John Dimaio,Bernard Gibbs,Jean Lefebvre,Yasuo Konishi,Debra Munn,Shi Yi Yue,Wilfried Hornberger |发布日期:1992.9 摘要:Described. The Substitution Of The Scissile Amide Function By A Ketomethylene Group Is Compatible With The Enzyme Active Site And Conferred Complete Plasma Proteolytic Stability. This Modification Also Enhanced Enzyme Affinity Up To 20-Fold With Hirutonin-4 (Iib, N = 4) Displaying Highest Affinity (Ki = 140 +/- 20 Pm). Hirutonins 1-4 Exhibited Potent Inhibition Of Plasma Prothrombin Time (Pt) And Activated