A macrocyclic coumarin-containing tripeptide via CuAAC chemistry

SS van Berkel, B van der Lee, FL van Delft…

文献索引：Van Berkel, Sander S.; Van Der Lee, Bas; Van Delft, Floris L.; Rutjes, Floris P. J. T. Chemical Communications, 2009 , # 28 p. 4272 - 4274

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被引用次数: 3

摘要

We envisaged a fluorophore-containing cyclic structure (ie2, Fig. 1) as a compelling strategy to (a) overcome the poor solubility of AMC in physiological media and (b) give rise to improved kinetic parameters. Constraining the linear peptide H-Gly-Pro-Arg-AMC in a bulky macrocyclic conformation is expected to hamper the entry into the thrombin active site, thus decreasing the affinity of the substrate for the binding pocket of thrombin resulting in favourable kinetic ...