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Macrocyclic inhibitors of 3C and 3C-like proteases of picornavirus, norovirus, and coronavirus

Authors
Journal
Bioorganic & Medicinal Chemistry Letters
0960-894X
Publisher
Elsevier
Publication Date
Volume
23
Issue
13
Identifiers
DOI: 10.1016/j.bmcl.2013.05.021
Keywords
  • Macrocyclic Inhibitors
  • 3C And 3Cl Proteases
  • Picornavirus-Like Supercluster Pathogens
Disciplines
  • Design

Abstract

Abstract The design, synthesis, and in vitro evaluation of the first macrocyclic inhibitor of 3C and 3C-like proteases of picornavirus, norovirus, and coronavirus are reported. The in vitro inhibitory activity (50% effective concentration) of the macrocyclic inhibitor toward enterovirus 3C protease (CVB3 Nancy strain), and coronavirus (SARS-CoV) and norovirus 3C-like proteases, was determined to be 1.8, 15.5 and 5.1μM, respectively.

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