Macrocyclic inhibitors of 3C and 3C-like proteases of picornavirus,norovirus, and coronavirus |
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| Authors: | Sivakoteswara Rao Mandadapu Pathum M. Weerawarna Allan M. Prior Roxanne Adeline Z. Uy Sridhar Aravapalli Kevin R. Alliston Gerald H. Lushington Yunjeong Kim Duy H. Hua Kyeong-Ok Chang William C. Groutas |
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| Affiliation: | 1. Department of Chemistry, Wichita State University, Wichita, KS 67260, USA;2. Department of Chemistry, Kansas State University, Manhattan, KS 66506, USA;3. LiS Consulting, Lawrence, KS 66046, USA;4. Department of Diagnostic Medicine/Pathobiology, College of Veterinary Medicine, Kansas State University, Manhattan, KS 66506, USA |
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| 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 5.1 μM, respectively. |
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| Keywords: | Macrocyclic inhibitors 3C and 3CL proteases Picornavirus-like supercluster pathogens |
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