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New developments for the design, synthesis and biological evaluation of potent SARS-CoV 3CLpro inhibitors

Identifieur interne : 002F22 ( Main/Exploration ); précédent : 002F21; suivant : 002F23

New 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 :

RBID : Pascal:09-0329242

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English descriptors

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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<name sortKey="Hayashi, Yoshio" sort="Hayashi, Yoshio" uniqKey="Hayashi Y" first="Yoshio" last="Hayashi">Yoshio Hayashi</name>
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<name sortKey="Kiso, Yoshiaki" sort="Kiso, Yoshiaki" uniqKey="Kiso Y" first="Yoshiaki" last="Kiso">Yoshiaki Kiso</name>
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<title level="j" type="main">Bioorganic & medicinal chemistry letters : (Print)</title>
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<keywords scheme="KwdEn" xml:lang="en">
<term>Antiviral</term>
<term>Biological activity</term>
<term>Chemical synthesis</term>
<term>Cysteine endopeptidases</term>
<term>Dipeptides</term>
<term>Enzyme inhibitor</term>
<term>Fluorine Organic compounds</term>
<term>In vitro</term>
<term>Modeling</term>
<term>Molecular dynamics method</term>
<term>Peptides</term>
<term>Protease inhibitor</term>
<term>Pyrrolidone derivatives</term>
<term>Severe acute respiratory syndrome virus</term>
<term>Thiazole derivatives</term>
<term>Valine derivatives</term>
</keywords>
<keywords scheme="Pascal" xml:lang="fr">
<term>Synthèse chimique</term>
<term>Activité biologique</term>
<term>Antiviral</term>
<term>Virus syndrome respiratoire aigu sévère</term>
<term>Inhibiteur protease</term>
<term>Cysteine endopeptidases</term>
<term>Dipeptide</term>
<term>In vitro</term>
<term>Méthode dynamique moléculaire</term>
<term>Dérivé du thiazole</term>
<term>Dérivé de la pyrrolidinone</term>
<term>Valine dérivé</term>
<term>Fluor Composé organique</term>
<term>Inhibiteur enzyme</term>
<term>Modélisation</term>
<term>Peptide</term>
<term>Leucinamide(benzyloxycarbonylvalyl-N-[2-(2-oxopyrrolidin-3-yl)-1-(thiazol-2-ylcarbonyl)éthyl])</term>
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<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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