SrasV1, Main, Exploration, bibRecord, 002A66

New developments for the design, synthesis and biological evaluation of potent SARS-CoV 3CL(pro) inhibitors.

Identifieur interne : 002A66 ( Main/Exploration ); précédent : 002A65; suivant : 002A67

New developments for the design, synthesis and biological evaluation of potent SARS-CoV 3CL(pro) inhibitors.

Auteurs : Thomas Regnier [Japon] ; Diganta Sarma ; Koushi Hidaka ; Usman Bacha ; Ernesto Freire ; Yoshio Hayashi ; Yoshiaki Kiso

Source :

Bioorganic & medicinal chemistry letters [ 1464-3405 ] ; 2009.

RBID : pubmed:19362479

Descripteurs français

KwdFr :
- Antiviraux (), Antiviraux (pharmacologie), Antiviraux (synthèse chimique), Benzothiazoles (), Benzothiazoles (pharmacologie), Benzothiazoles (synthèse chimique), Chymases (antagonistes et inhibiteurs), Chymases (métabolisme), Conception de médicament, Cysteine endopeptidases (métabolisme), Cétones (), Cétones (synthèse chimique), Inhibiteurs de protéases (), Inhibiteurs de protéases (pharmacologie), Inhibiteurs de protéases (synthèse chimique), Peptides (), Peptides (pharmacologie), Peptides (synthèse chimique), Protéines virales (antagonistes et inhibiteurs), Protéines virales (métabolisme), Pyrrolidones (), Pyrrolidones (pharmacologie), Pyrrolidones (synthèse chimique), Relation structure-activité, Simulation numérique, Séquence d'acides aminés, Thiazoles (), Thiazoles (pharmacologie), Thiazoles (synthèse chimique), Virus du SRAS.
MESH :
- antagonistes et inhibiteurs : Chymases, Protéines virales.
- métabolisme : Chymases, Cysteine endopeptidases, Protéines virales.
- pharmacologie : Antiviraux, Benzothiazoles, Inhibiteurs de protéases, Peptides, Pyrrolidones, Thiazoles.
- synthèse chimique : Antiviraux, Benzothiazoles, Cétones, Inhibiteurs de protéases, Peptides, Pyrrolidones, Thiazoles.
- Antiviraux, Benzothiazoles, Conception de médicament, Cétones, Inhibiteurs de protéases, Peptides, Pyrrolidones, Relation structure-activité, Simulation numérique, Séquence d'acides aminés, Thiazoles, Virus du SRAS.

English descriptors

KwdEn :
- Amino Acid Sequence, Antiviral Agents (chemical synthesis), Antiviral Agents (chemistry), Antiviral Agents (pharmacology), Benzothiazoles (chemical synthesis), Benzothiazoles (chemistry), Benzothiazoles (pharmacology), Chymases (antagonists & inhibitors), Chymases (metabolism), Computer Simulation, Cysteine Endopeptidases (metabolism), Drug Design, Ketones (chemical synthesis), Ketones (chemistry), Peptides (chemical synthesis), Peptides (chemistry), Peptides (pharmacology), Protease Inhibitors (chemical synthesis), Protease Inhibitors (chemistry), Protease Inhibitors (pharmacology), Pyrrolidinones (chemical synthesis), Pyrrolidinones (chemistry), Pyrrolidinones (pharmacology), SARS Virus, Structure-Activity Relationship, Thiazoles (chemical synthesis), Thiazoles (chemistry), Thiazoles (pharmacology), Viral Proteins (antagonists & inhibitors), Viral Proteins (metabolism).
MESH :
- chemical , antagonists & inhibitors : Chymases, Viral Proteins.
- chemical , chemical synthesis : Antiviral Agents, Benzothiazoles, Ketones, Peptides, Protease Inhibitors, Pyrrolidinones, Thiazoles.
- chemical , chemistry : Antiviral Agents, Benzothiazoles, Ketones, Peptides, Protease Inhibitors, Pyrrolidinones, Thiazoles.
- chemical , metabolism : Chymases, Cysteine Endopeptidases, Viral Proteins.
- chemical , pharmacology : Antiviral Agents, Benzothiazoles, Peptides, Protease Inhibitors, Pyrrolidinones, Thiazoles.
- Amino Acid Sequence, Computer Simulation, Drug Design, SARS Virus, Structure-Activity Relationship.

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.

DOI: 10.1016/j.bmcl.2009.03.118
PubMed: 19362479

Affiliations:

Japon

Le document en format XML

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<author><name sortKey="Regnier, Thomas" sort="Regnier, Thomas" uniqKey="Regnier T" first="Thomas" last="Regnier">Thomas Regnier</name>
<affiliation wicri:level="1"><nlm:affiliation>Department of Medicinal Chemistry, Center for Frontier Research in Medicinal Science, Kyoto Pharmaceutical University, Japan.</nlm:affiliation>
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<wicri:regionArea>Department of Medicinal Chemistry, Center for Frontier Research in Medicinal Science, Kyoto Pharmaceutical University</wicri:regionArea>
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<author><name sortKey="Hidaka, Koushi" sort="Hidaka, Koushi" uniqKey="Hidaka K" first="Koushi" last="Hidaka">Koushi Hidaka</name>
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<author><name sortKey="Bacha, Usman" sort="Bacha, Usman" uniqKey="Bacha U" first="Usman" last="Bacha">Usman Bacha</name>
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<author><name sortKey="Freire, Ernesto" sort="Freire, Ernesto" uniqKey="Freire E" first="Ernesto" last="Freire">Ernesto Freire</name>
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<author><name sortKey="Hayashi, Yoshio" sort="Hayashi, Yoshio" uniqKey="Hayashi Y" first="Yoshio" last="Hayashi">Yoshio Hayashi</name>
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<term>Antiviral Agents (chemistry)</term>
<term>Antiviral Agents (pharmacology)</term>
<term>Benzothiazoles (chemical synthesis)</term>
<term>Benzothiazoles (chemistry)</term>
<term>Benzothiazoles (pharmacology)</term>
<term>Chymases (antagonists & inhibitors)</term>
<term>Chymases (metabolism)</term>
<term>Computer Simulation</term>
<term>Cysteine Endopeptidases (metabolism)</term>
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<term>Ketones (chemistry)</term>
<term>Peptides (chemical synthesis)</term>
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<term>Peptides (pharmacology)</term>
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<term>Protease Inhibitors (chemistry)</term>
<term>Protease Inhibitors (pharmacology)</term>
<term>Pyrrolidinones (chemical synthesis)</term>
<term>Pyrrolidinones (chemistry)</term>
<term>Pyrrolidinones (pharmacology)</term>
<term>SARS Virus</term>
<term>Structure-Activity Relationship</term>
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<term>Thiazoles (chemistry)</term>
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<term>Chymases (métabolisme)</term>
<term>Conception de médicament</term>
<term>Cysteine endopeptidases (métabolisme)</term>
<term>Cétones ()</term>
<term>Cétones (synthèse chimique)</term>
<term>Inhibiteurs de protéases ()</term>
<term>Inhibiteurs de protéases (pharmacologie)</term>
<term>Inhibiteurs de protéases (synthèse chimique)</term>
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<term>Peptides (pharmacologie)</term>
<term>Peptides (synthèse chimique)</term>
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<term>Protéines virales (métabolisme)</term>
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<term>Pyrrolidones (pharmacologie)</term>
<term>Pyrrolidones (synthèse chimique)</term>
<term>Relation structure-activité</term>
<term>Simulation numérique</term>
<term>Séquence d'acides aminés</term>
<term>Thiazoles ()</term>
<term>Thiazoles (pharmacologie)</term>
<term>Thiazoles (synthèse chimique)</term>
<term>Virus du SRAS</term>
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<term>Benzothiazoles</term>
<term>Ketones</term>
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<term>Protease Inhibitors</term>
<term>Pyrrolidinones</term>
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<term>Protease Inhibitors</term>
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<term>Thiazoles</term>
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<term>Cysteine Endopeptidases</term>
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<term>Peptides</term>
<term>Protease Inhibitors</term>
<term>Pyrrolidinones</term>
<term>Thiazoles</term>
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<keywords scheme="MESH" qualifier="antagonistes et inhibiteurs" xml:lang="fr"><term>Chymases</term>
<term>Protéines virales</term>
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<term>Cysteine endopeptidases</term>
<term>Protéines virales</term>
</keywords>
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<term>Inhibiteurs de protéases</term>
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<term>Thiazoles</term>
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<term>Inhibiteurs de protéases</term>
<term>Peptides</term>
<term>Pyrrolidones</term>
<term>Thiazoles</term>
</keywords>
<keywords scheme="MESH" xml:lang="en"><term>Amino Acid Sequence</term>
<term>Computer Simulation</term>
<term>Drug Design</term>
<term>SARS Virus</term>
<term>Structure-Activity Relationship</term>
</keywords>
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<term>Inhibiteurs de protéases</term>
<term>Peptides</term>
<term>Pyrrolidones</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>
</front>
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<tree><noCountry><name sortKey="Bacha, Usman" sort="Bacha, Usman" uniqKey="Bacha U" first="Usman" last="Bacha">Usman Bacha</name>
<name sortKey="Freire, Ernesto" sort="Freire, Ernesto" uniqKey="Freire E" first="Ernesto" last="Freire">Ernesto Freire</name>
<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>
<name sortKey="Sarma, Diganta" sort="Sarma, Diganta" uniqKey="Sarma D" first="Diganta" last="Sarma">Diganta Sarma</name>
</noCountry>
<country name="Japon"><noRegion><name sortKey="Regnier, Thomas" sort="Regnier, Thomas" uniqKey="Regnier T" first="Thomas" last="Regnier">Thomas Regnier</name>
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Serveur d'exploration SRAS

New developments for the design, synthesis and biological evaluation of potent SARS-CoV 3CL(pro) inhibitors.

New developments for the design, synthesis and biological evaluation of potent SARS-CoV 3CL(pro) inhibitors.

Source :

Descripteurs français

English descriptors

Abstract

Links toward previous steps (curation, corpus...)

Le document en format XML

Pour manipuler ce document sous Unix (Dilib)

Pour mettre un lien sur cette page dans le réseau Wicri

Pour générer des pages wiki

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