174960-95-3Relevant academic research and scientific papers
Novel, potent non-covalent thrombin inhibitors incorporating P3-lactam scaffolds
Ho, Jonathan Z.,Gibson, Tony S.,Semple
, p. 743 - 748 (2007/10/03)
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.
