Bioorganic and Medicinal Chemistry Letters
Bioorganic and Medicinal Chemistry Letters
5 years ago

Structure-based design and synthesis of macrocyclic human rhinovirus 3C protease inhibitors.

Structure-based design and synthesis of macrocyclic human rhinovirus 3C protease inhibitors.
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.

Publisher URL: www.sciencedirect.com/science

DOI: S0960894X18300751

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