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About:
Macrocyclic Inhibitors of 3C and 3C-like Proteases of Picornavirus, Norovirus, and Coronavirus
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An Entity of Type :
schema:ScholarlyArticle
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wasabi.inria.fr
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Type:
Academic Article
research paper
schema:ScholarlyArticle
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type
Academic Article
research paper
schema:ScholarlyArticle
isDefinedBy
Covid-on-the-Web dataset
has title
Macrocyclic Inhibitors of 3C and 3C-like Proteases of Picornavirus, Norovirus, and Coronavirus
Creator
Chang, William
Alliston, Gerald
Aravapalli, Kevin
Groutas,
Hua, Kyeong-Ok
Kim, Duy
Lushington, Yunjeong
Mandadapu, Pathum
Prior, Roxanne
Sivakoteswara, Rao
Uy, Sridhar
Weerawarna, Allan
Source
Elsevier; Medline; PMC
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.
has issue date
2013-07-01
(
xsd:dateTime
)
bibo:doi
10.1016/j.bmcl.2013.05.021
bibo:pmid
23727045
has license
bronze-oa
sha1sum (hex)
119d76e13a16297a7a15446e2d75fe72c9153230
schema:url
https://doi.org/10.1016/j.bmcl.2013.05.021
resource representing a document's title
Macrocyclic Inhibitors of 3C and 3C-like Proteases of Picornavirus, Norovirus, and Coronavirus
has PubMed Central identifier
PMC3750990
has PubMed identifier
23727045
schema:publication
Bioorganic & Medicinal Chemistry Letters
resource representing a document's body
covid:119d76e13a16297a7a15446e2d75fe72c9153230#body_text
is
schema:about
of
named entity 'norovirus'
named entity 'Macrocyclic'
named entity 'coronavirus'
named entity 'INHIBITORS'
named entity 'NOROVIRUS'
named entity 'LIKE'
named entity 'CORONAVIRUS'
named entity 'PROTEASES'
named entity 'PICORNAVIRUS'
named entity 'Cbz'
named entity 'arginine'
named entity 'cationic'
named entity 'proteases'
named entity 'coronavirus'
named entity 'proteases'
named entity 'THF'
named entity 'alkyl azide'
named entity 'coronavirus'
named entity 'protease'
named entity 'SARS-CoV'
named entity 'proteolytic processing'
named entity 'aqueous'
named entity 'LiOH'
named entity 'alcohol'
named entity 'N-terminal'
named entity 'PyMol'
named entity 'macrocyclic'
named entity 'protein data bank'
named entity 'chymotrypsin-like'
named entity 'conformation'
named entity 'protective group'
named entity 'norovirus'
named entity 'Cbz'
named entity 'virus replication'
named entity 'Cys'
named entity 'substrate specificity'
named entity 'effective concentration'
named entity 'receptor'
named entity '3C protease'
named entity 'HCl'
named entity 'aldehyde'
named entity 'Glu'
named entity 'ligands'
named entity 'aspartate'
named entity 'positive sense'
named entity 'Cyclization'
named entity 'macrocyclic'
named entity 'ester'
named entity 'Pymol'
named entity 'macrocyclization'
named entity 'macrocyclic'
named entity 'receptor binding'
named entity '3CLpro'
named entity 'inhibitory activity'
named entity 'picornavirus'
named entity 'binding site'
named entity 'Boc protecting group'
named entity 'HOBt'
named entity 'picornavirus'
named entity 'coronavirus'
named entity 'SARS-CoV'
named entity 'proteolytic processing'
named entity 'isobutyl group'
named entity 'dioxane'
named entity 'Cys'
named entity 'protonating'
named entity 'polyprotein'
named entity 'active site'
named entity 'viral pathogens'
named entity 'genetic diversity'
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