Macrocyclic inhibitors of 3C and 3C-like proteases of picornavirus, norovirus, and coronavirus.
Identifieur interne : 001189 ( PubMed/Corpus ); précédent : 001188; suivant : 001190Macrocyclic inhibitors of 3C and 3C-like proteases of picornavirus, norovirus, and coronavirus.
Auteurs : 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. GroutasSource :
- Bioorganic & medicinal chemistry letters [ 1464-3405 ] ; 2013.
English descriptors
- KwdEn :
- Coronavirus (enzymology), Dose-Response Relationship, Drug, Drug Design, Macrocyclic Compounds (chemical synthesis), Macrocyclic Compounds (chemistry), Macrocyclic Compounds (pharmacology), Models, Molecular, Molecular Conformation, Norovirus (enzymology), Peptide Hydrolases (metabolism), Picornaviridae (enzymology), Protease Inhibitors (chemical synthesis), Protease Inhibitors (chemistry), Protease Inhibitors (pharmacology), Structure-Activity Relationship.
- MESH :
- chemical , chemical synthesis : Macrocyclic Compounds, Protease Inhibitors.
- chemical , chemistry : Macrocyclic Compounds, Protease Inhibitors.
- enzymology : Coronavirus, Norovirus, Picornaviridae.
- chemical , metabolism : Peptide Hydrolases.
- chemical , pharmacology : Macrocyclic Compounds, Protease Inhibitors.
- Dose-Response Relationship, Drug, Drug Design, Models, Molecular, Molecular Conformation, Structure-Activity Relationship.
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.
DOI: 10.1016/j.bmcl.2013.05.021
PubMed: 23727045
Links to Exploration step
pubmed:23727045Le document en format XML
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<front><div type="abstract" xml:lang="en">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.</div>
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