Bioorganic & medicinal chemistry letters

Novel, Potent Non-Covalent Thrombin Inhibitors Incorporating P 3-Lactam Scaffolds

JZ Ho, TS Gibson, JE Semple

文献索引：Ho, Jonathan Z.; Gibson, Tony S.; Semple Bioorganic and Medicinal Chemistry Letters, 2002 , vol. 12, # 5 p. 743 - 748

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被引用次数: 30

摘要

Evolution of P1-argininal inhibitor prototypes led to a series of non-covalent P3-7-membered lactam inhibitors 1a–w, featuring novel peptidomimetic units that probe each of the S1, S2, and S3 specificity pockets of thrombin. Rigid P1-arginine surrogates possessing a wide range of basicity (calcd pKa's∼ neutral–14) were surveyed. The design, synthesis, and biological activity of these targets are presented.