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  • Title: Structure-based design and synthesis of macrocyclic human rhinovirus 3C protease inhibitors.
    Author: Namoto K, Sirockin F, Sellner H, Wiesmann C, Villard F, Moreau RJ, Valeur E, Paulding SC, Schleeger S, Schipp K, Loup J, Andrews L, Swale R, Robinson M, Farady CJ.
    Journal: Bioorg Med Chem Lett; 2018 Mar 01; 28(5):906-909. PubMed ID: 29433930.
    Abstract:
    The design and synthesis of macrocyclic inhibitors of human rhinovirus 3C protease is described. A macrocyclic linkage of the P1 and P3 residues, and the subsequent structure-based optimization of the macrocycle conformation and size led to the identification of a potent biochemical inhibitor 10 with sub-micromolar antiviral activity.
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