Design and Synthesis of Peptidomimetic Severe Acute Respiratory Syndrome Chymotrypsin-like Protease Inhibitors
Identifieur interne : 001006 ( Main/Exploration ); précédent : 001005; suivant : 001007Design 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.
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.
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DOI: 10.1021/jm050548m
Affiliations:
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Rota</name><affiliation wicri:level="1"><country xml:lang="fr">Géorgie (pays)</country><wicri:regionArea>Departments of Chemistry and Medicinal Chemistry,Purdue University, West Lafayette, Indiana 47907,Department of Chemistry, University of Illinois at Chicago,Chicago, Illinois 60607, Center for PharmaceuticalBiotechnology and Department of Medicinal Chemistry andPharmacognosy, University of Illinois at Chicago, 900 S.Ashland, Illinois 60607, Department of Microbiology andImmunology, Loyola University of Chicago, Stritch School ofMedicine, Maywood, Illinois, and Center for Disease Controland Prevention, Atlanta</wicri:regionArea><wicri:noRegion>Atlanta</wicri:noRegion></affiliation><affiliation></affiliation></author><author><name sortKey="Baker, Susan C" sort="Baker, Susan C" uniqKey="Baker S" first="Susan C." last="Baker">Susan C. Baker</name><affiliation wicri:level="1"><country xml:lang="fr">Géorgie (pays)</country><wicri:regionArea>Departments of Chemistry and Medicinal Chemistry,Purdue University, West Lafayette, Indiana 47907,Department of Chemistry, University of Illinois at Chicago,Chicago, Illinois 60607, Center for PharmaceuticalBiotechnology and Department of Medicinal Chemistry andPharmacognosy, University of Illinois at Chicago, 900 S.Ashland, Illinois 60607, Department of Microbiology andImmunology, Loyola University of Chicago, Stritch School ofMedicine, Maywood, Illinois, and Center for Disease Controland Prevention, Atlanta</wicri:regionArea><wicri:noRegion>Atlanta</wicri:noRegion></affiliation><affiliation></affiliation></author><author><name sortKey="Johnson, Michael E" sort="Johnson, Michael E" uniqKey="Johnson M" first="Michael E." last="Johnson">Michael E. Johnson</name><affiliation wicri:level="1"><country xml:lang="fr">Géorgie (pays)</country><wicri:regionArea>Departments of Chemistry and Medicinal Chemistry,Purdue University, West Lafayette, Indiana 47907,Department of Chemistry, University of Illinois at Chicago,Chicago, Illinois 60607, Center for PharmaceuticalBiotechnology and Department of Medicinal Chemistry andPharmacognosy, University of Illinois at Chicago, 900 S.Ashland, Illinois 60607, Department of Microbiology andImmunology, Loyola University of Chicago, Stritch School ofMedicine, Maywood, Illinois, and Center for Disease Controland Prevention, Atlanta</wicri:regionArea><wicri:noRegion>Atlanta</wicri:noRegion></affiliation><affiliation></affiliation></author><author><name sortKey="Mesecar, Andrew D" sort="Mesecar, Andrew D" uniqKey="Mesecar A" first="Andrew D." last="Mesecar">Andrew D. Mesecar</name><affiliation wicri:level="1"><country xml:lang="fr">Géorgie (pays)</country><wicri:regionArea>Departments of Chemistry and Medicinal Chemistry,Purdue University, West Lafayette, Indiana 47907,Department of Chemistry, University of Illinois at Chicago,Chicago, Illinois 60607, Center for PharmaceuticalBiotechnology and Department of Medicinal Chemistry andPharmacognosy, University of Illinois at Chicago, 900 S.Ashland, Illinois 60607, Department of Microbiology andImmunology, Loyola University of Chicago, Stritch School ofMedicine, Maywood, Illinois, and Center for Disease Controland Prevention, Atlanta</wicri:regionArea><wicri:noRegion>Atlanta</wicri:noRegion></affiliation><affiliation></affiliation></author></analytic><monogr></monogr><series><title level="j" type="main">Journal of Medicinal Chemistry</title><title level="j" type="abbrev">J. Med. Chem.</title><idno type="ISSN">0022-2623</idno><idno type="eISSN">1520-4804</idno><imprint><publisher>American Chemical Society</publisher><date type="e-published" when="2005-10-04">2005</date><date when="2005-11-03">2005</date><biblScope unit="vol">48</biblScope><biblScope unit="issue">22</biblScope><biblScope unit="page" from="6767">6767</biblScope><biblScope unit="page" to="6771">6771</biblScope></imprint><idno type="ISSN">0022-2623</idno></series></biblStruct></sourceDesc><seriesStmt><idno type="ISSN">0022-2623</idno></seriesStmt></fileDesc><profileDesc><textClass></textClass></profileDesc></teiHeader><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></list><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></tree></affiliations></record>Pour manipuler ce document sous Unix (Dilib)
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