SrasV1, Main, Exploration, bibRecord, 004A02

Design and Synthesis of Peptidomimetic Severe Acute Respiratory Syndrome Chymotrypsin-like Protease Inhibitors

Identifieur interne : 004A02 ( Main/Exploration ); précédent : 004A01; suivant : 004A03

Design and Synthesis of Peptidomimetic Severe Acute Respiratory Syndrome Chymotrypsin-like Protease Inhibitors

Auteurs : Arun K. Ghosh [Géorgie (pays), États-Unis] ; Kai Xi [Géorgie (pays), États-Unis] ; Kiira Ratia [Géorgie (pays)] ; Bernard D. Santarsiero [Géorgie (pays)] ; Wentao Fu [Géorgie (pays)] ; Brian H. Harcourt [Géorgie (pays)] ; Paul A. Rota [Géorgie (pays)] ; Susan C. Baker [Géorgie (pays)] ; Michael E. Johnson [Géorgie (pays)] ; Andrew D. Mesecar [Géorgie (pays)]

Source :

Journal of Medicinal Chemistry [ 0022-2623 ] ; 2005.

RBID : ISTEX:AD6693F86E9D863C197B903A7B71C09B78082110

Descripteurs français

English descriptors

KwdEn :
- Animals, Antiviral, Antiviral Agents (chemical synthesis), Antiviral Agents (chemistry), Antiviral Agents (pharmacology), Biological activity, Carboxamide, Cells, Cultured, Chemical synthesis, Chymases, Crystallography, X-Ray, Dipeptides (chemistry), Drug Design, Enzyme inhibitor, Humans, In vitro, Inhibitor enzyme complex, Isoxazoles (chemical synthesis), Isoxazoles (chemistry), Isoxazoles (pharmacology), Ketoamide, Kinetics, Lactam, Lactams (chemical synthesis), Lactams (chemistry), Lactams (pharmacology), Modeling, Models, Molecular, Molecular Mimicry, Molecular model, Nitrogen heterocycle, Non peptide compound, Oxygen nitrogen heterocycle, Peptidases, Peptides (chemistry), Peptidomimetic compound, Protease inhibitor, SARS Virus (drug effects), SARS Virus (enzymology), Serine Endopeptidases (chemistry), Serine Endopeptidases (metabolism), Serine Proteinase Inhibitors (chemical synthesis), Serine Proteinase Inhibitors (chemistry), Serine Proteinase Inhibitors (pharmacology), Severe acute respiratory syndrome virus, Stereoisomerism, Structure-Activity Relationship, Vinylic compound.
MESH :
- chemical , chemical synthesis : Antiviral Agents, Isoxazoles, Lactams, Serine Proteinase Inhibitors.
- chemical , chemistry : Antiviral Agents, Dipeptides, Isoxazoles, Lactams, Peptides, Serine Endopeptidases, Serine Proteinase Inhibitors.
- chemical , metabolism : Serine Endopeptidases.
- chemical , pharmacology : Antiviral Agents, Isoxazoles, Lactams, Serine Proteinase Inhibitors.
- drug effects : SARS Virus.
- enzymology : SARS Virus.
- Animals, Cells, Cultured, Chymases, Crystallography, X-Ray, Drug Design, Humans, Kinetics, Models, Molecular, Molecular Mimicry, Stereoisomerism, Structure-Activity Relationship.

Abstract

Design, synthesis, and biological evaluation of peptidomimetic severe acute respiratory syndrome chymotrypsin-like protease (SARS-3CLpro) inhibitors for severe acute respiratory syndrome coronavirus (SARS-CoV) are described. These inhibitors exhibited antiviral activity against SARS-CoV in infected cells in the micromolar range. An X-ray crystal structure of our lead inhibitor (4) bound to SARS-3CLpro provided important drug-design templates for the design of small-molecule inhibitors.

Url:

https://api.istex.fr/ark:/67375/TPS-WHX6D4F8-M/fulltext.pdf

DOI: 10.1021/jm050548m

Affiliations:

Le document en format XML

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<term>Antiviral</term>
<term>Antiviral Agents (chemical synthesis)</term>
<term>Antiviral Agents (chemistry)</term>
<term>Antiviral Agents (pharmacology)</term>
<term>Biological activity</term>
<term>Carboxamide</term>
<term>Cells, Cultured</term>
<term>Chemical synthesis</term>
<term>Chymases</term>
<term>Crystallography, X-Ray</term>
<term>Dipeptides (chemistry)</term>
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<term>Enzyme inhibitor</term>
<term>Humans</term>
<term>In vitro</term>
<term>Inhibitor enzyme complex</term>
<term>Isoxazoles (chemical synthesis)</term>
<term>Isoxazoles (chemistry)</term>
<term>Isoxazoles (pharmacology)</term>
<term>Ketoamide</term>
<term>Kinetics</term>
<term>Lactam</term>
<term>Lactams (chemical synthesis)</term>
<term>Lactams (chemistry)</term>
<term>Lactams (pharmacology)</term>
<term>Modeling</term>
<term>Models, Molecular</term>
<term>Molecular Mimicry</term>
<term>Molecular model</term>
<term>Nitrogen heterocycle</term>
<term>Non peptide compound</term>
<term>Oxygen nitrogen heterocycle</term>
<term>Peptidases</term>
<term>Peptides (chemistry)</term>
<term>Peptidomimetic compound</term>
<term>Protease inhibitor</term>
<term>SARS Virus (drug effects)</term>
<term>SARS Virus (enzymology)</term>
<term>Serine Endopeptidases (chemistry)</term>
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<term>Serine Proteinase Inhibitors (chemistry)</term>
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</keywords>
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<term>Antiviraux (pharmacologie)</term>
<term>Antiviraux (synthèse chimique)</term>
<term>Cellules cultivées</term>
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<term>Cinétique</term>
<term>Conception de médicament</term>
<term>Cristallographie aux rayons X</term>
<term>Dipeptides ()</term>
<term>Humains</term>
<term>Inhibiteurs de la sérine protéinase ()</term>
<term>Inhibiteurs de la sérine protéinase (pharmacologie)</term>
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<term>Lactames (synthèse chimique)</term>
<term>Mimétisme moléculaire</term>
<term>Modèles moléculaires</term>
<term>Peptides ()</term>
<term>Relation structure-activité</term>
<term>Serine endopeptidases ()</term>
<term>Serine endopeptidases (métabolisme)</term>
<term>Stéréoisomérie</term>
<term>Virus du SRAS ()</term>
<term>Virus du SRAS (enzymologie)</term>
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<keywords scheme="MESH" type="chemical" qualifier="chemical synthesis" xml:lang="en"><term>Antiviral Agents</term>
<term>Isoxazoles</term>
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<keywords scheme="MESH" type="chemical" qualifier="chemistry" xml:lang="en"><term>Antiviral Agents</term>
<term>Dipeptides</term>
<term>Isoxazoles</term>
<term>Lactams</term>
<term>Peptides</term>
<term>Serine Endopeptidases</term>
<term>Serine Proteinase Inhibitors</term>
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<keywords scheme="MESH" type="chemical" qualifier="metabolism" xml:lang="en"><term>Serine Endopeptidases</term>
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<keywords scheme="MESH" type="chemical" qualifier="pharmacology" xml:lang="en"><term>Antiviral Agents</term>
<term>Isoxazoles</term>
<term>Lactams</term>
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<keywords scheme="MESH" qualifier="enzymology" xml:lang="en"><term>SARS Virus</term>
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<keywords scheme="MESH" qualifier="pharmacologie" xml:lang="fr"><term>Antiviraux</term>
<term>Inhibiteurs de la sérine protéinase</term>
<term>Isoxazoles</term>
<term>Lactames</term>
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<keywords scheme="MESH" qualifier="synthèse chimique" xml:lang="fr"><term>Antiviraux</term>
<term>Inhibiteurs de la sérine protéinase</term>
<term>Isoxazoles</term>
<term>Lactames</term>
</keywords>
<keywords scheme="MESH" xml:lang="en"><term>Animals</term>
<term>Cells, Cultured</term>
<term>Chymases</term>
<term>Crystallography, X-Ray</term>
<term>Drug Design</term>
<term>Humans</term>
<term>Kinetics</term>
<term>Models, Molecular</term>
<term>Molecular Mimicry</term>
<term>Stereoisomerism</term>
<term>Structure-Activity Relationship</term>
</keywords>
<keywords scheme="MESH" xml:lang="fr"><term>Animaux</term>
<term>Antiviraux</term>
<term>Cellules cultivées</term>
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<term>Composé non peptide</term>
<term>Composé peptidomimétique</term>
<term>Composé vinylique</term>
<term>Cétoamide</term>
<term>Hétérocycle azote</term>
<term>Hétérocycle oxygène azote</term>
<term>In vitro</term>
<term>Inhibiteur enzyme</term>
<term>Inhibiteur protease</term>
<term>Isoxazole-3-carboxamide dérivé</term>
<term>Lactame</term>
<term>Modèle moléculaire</term>
<term>Modélisation</term>
<term>Peptidases</term>
<term>Pyrrolidin-2-one dérivé</term>
<term>Pyrrolidine-3-pent-2-énoïque acide(γ-[(5-méthyl-2-[4-méthyl-3-([(5-méthylisoxazol-3-yl)carbonyl]amino)-2-oxopentyl]hex-4-énoyl)amino]-2-oxo) ester éthyle</term>
<term>Synthèse chimique</term>
<term>Virus syndrome respiratoire aigu sévère</term>
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<front><div type="abstract">Design, synthesis, and biological evaluation of peptidomimetic severe acute respiratory syndrome chymotrypsin-like protease (SARS-3CLpro) inhibitors for severe acute respiratory syndrome coronavirus (SARS-CoV) are described. These inhibitors exhibited antiviral activity against SARS-CoV in infected cells in the micromolar range. An X-ray crystal structure of our lead inhibitor (4) bound to SARS-3CLpro provided important drug-design templates for the design of small-molecule inhibitors.</div>
</front>
</TEI>
<affiliations><list><country><li>Géorgie (pays)</li>
<li>États-Unis</li>
</country>
<region><li>Illinois</li>
</region>
<settlement><li>Chicago</li>
</settlement>
<orgName><li>Université de l'Illinois à Chicago</li>
</orgName>
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<tree><country name="Géorgie (pays)"><noRegion><name sortKey="Ghosh, Arun K" sort="Ghosh, Arun K" uniqKey="Ghosh A" first="Arun K." last="Ghosh">Arun K. Ghosh</name>
</noRegion>
<name sortKey="Baker, Susan C" sort="Baker, Susan C" uniqKey="Baker S" first="Susan C." last="Baker">Susan C. Baker</name>
<name sortKey="Fu, Wentao" sort="Fu, Wentao" uniqKey="Fu W" first="Wentao" last="Fu">Wentao Fu</name>
<name sortKey="Harcourt, Brian H" sort="Harcourt, Brian H" uniqKey="Harcourt B" first="Brian H." last="Harcourt">Brian H. Harcourt</name>
<name sortKey="Johnson, Michael E" sort="Johnson, Michael E" uniqKey="Johnson M" first="Michael E." last="Johnson">Michael E. Johnson</name>
<name sortKey="Mesecar, Andrew D" sort="Mesecar, Andrew D" uniqKey="Mesecar A" first="Andrew D." last="Mesecar">Andrew D. Mesecar</name>
<name sortKey="Ratia, Kiira" sort="Ratia, Kiira" uniqKey="Ratia K" first="Kiira" last="Ratia">Kiira Ratia</name>
<name sortKey="Rota, Paul A" sort="Rota, Paul A" uniqKey="Rota P" first="Paul A." last="Rota">Paul A. Rota</name>
<name sortKey="Santarsiero, Bernard D" sort="Santarsiero, Bernard D" uniqKey="Santarsiero B" first="Bernard D." last="Santarsiero">Bernard D. Santarsiero</name>
<name sortKey="Xi, Kai" sort="Xi, Kai" uniqKey="Xi K" first="Kai" last="Xi">Kai Xi</name>
</country>
<country name="États-Unis"><region name="Illinois"><name sortKey="Ghosh, Arun K" sort="Ghosh, Arun K" uniqKey="Ghosh A" first="Arun K." last="Ghosh">Arun K. Ghosh</name>
</region>
<name sortKey="Ghosh, Arun K" sort="Ghosh, Arun K" uniqKey="Ghosh A" first="Arun K." last="Ghosh">Arun K. Ghosh</name>
<name sortKey="Xi, Kai" sort="Xi, Kai" uniqKey="Xi K" first="Kai" last="Xi">Kai Xi</name>
</country>
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</affiliations>
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Design and Synthesis of Peptidomimetic Severe Acute Respiratory Syndrome Chymotrypsin-like Protease Inhibitors

Design and Synthesis of Peptidomimetic Severe Acute Respiratory Syndrome Chymotrypsin-like Protease Inhibitors

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