New developments for the design, synthesis and biological evaluation of potent SARS-CoV 3CLpro inhibitors
Identifieur interne : 002F22 ( Main/Exploration ); précédent : 002F21; suivant : 002F23New developments for the design, synthesis and biological evaluation of potent SARS-CoV 3CLpro inhibitors
Auteurs : Thomas Regnier [Japon] ; Diganta Sarma [Japon] ; Koushi Hidaka [Japon] ; Usman Bacha [États-Unis] ; Ernesto Freire [États-Unis] ; Yoshio Hayashi [Japon] ; Yoshiaki Kiso [Japon]Source :
- Bioorganic & medicinal chemistry letters : (Print) [ 0960-894X ] ; 2009.
Descripteurs français
- Pascal (Inist)
- Synthèse chimique, Activité biologique, Antiviral, Virus syndrome respiratoire aigu sévère, Inhibiteur protease, Cysteine endopeptidases, Dipeptide, In vitro, Méthode dynamique moléculaire, Dérivé du thiazole, Dérivé de la pyrrolidinone, Valine dérivé, Fluor Composé organique, Inhibiteur enzyme, Modélisation, Peptide, Leucinamide(benzyloxycarbonylvalyl-N-[2-(2-oxopyrrolidin-3-yl)-1-(thiazol-2-ylcarbonyl)éthyl]), Leucine dérivé.
English descriptors
- KwdEn :
- Antiviral, Biological activity, Chemical synthesis, Cysteine endopeptidases, Dipeptides, Enzyme inhibitor, Fluorine Organic compounds, In vitro, Modeling, Molecular dynamics method, Peptides, Protease inhibitor, Pyrrolidone derivatives, Severe acute respiratory syndrome virus, Thiazole derivatives, Valine derivatives.
Abstract
A series of trifluoromethyl, benzothiazolyl or thiazolyl ketone-containing peptidic compounds as SARS-CoV 3CL protease inhibitors were developed and their potency was evaluated by in vitro protease inhibitory assays. Three candidates had encouraging results for the development of new anti-SARS compounds.
Affiliations:
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Le document en format XML
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<term>Molecular dynamics method</term>
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<term>Cysteine endopeptidases</term>
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<front><div type="abstract" xml:lang="en">A series of trifluoromethyl, benzothiazolyl or thiazolyl ketone-containing peptidic compounds as SARS-CoV 3CL protease inhibitors were developed and their potency was evaluated by in vitro protease inhibitory assays. Three candidates had encouraging results for the development of new anti-SARS compounds.</div>
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