Synthesis and evaluation of isatin derivatives as effective SARS coronavirus 3CL protease inhibitors.
Identifieur interne : 000F53 ( Ncbi/Curation ); précédent : 000F52; suivant : 000F54Synthesis and evaluation of isatin derivatives as effective SARS coronavirus 3CL protease inhibitors.
Auteurs : Li-Rung Chen [République populaire de Chine] ; Yu-Chin Wang ; Yi Wen Lin ; Shan-Yen Chou ; Shyh-Fong Chen ; Lee Tai Liu ; Ying-Ta Wu ; Chih-Jung Kuo ; Tom Shieh-Shung Chen ; Shin-Hun JuangSource :
- Bioorganic & medicinal chemistry letters [ 0960-894X ] ; 2005.
Descripteurs français
- KwdFr :
- Activation enzymatique, Chymotrypsine (pharmacologie), Cysteine endopeptidases, Endopeptidases, Humains, Inhibiteurs de protéases (), Inhibiteurs de protéases (pharmacologie), Inhibiteurs de protéases (synthèse chimique), Isatine (analogues et dérivés), Isatine (pharmacologie), Isatine (synthèse chimique), Papaïne (pharmacologie), Protéines virales (antagonistes et inhibiteurs), Relation structure-activité, Simulation numérique, Sites de fixation, Spécificité du substrat, Structure moléculaire, Transfert d'énergie par résonance de fluorescence, Trypsine (pharmacologie), Virus du SRAS (enzymologie).
- MESH :
- analogues et dérivés : Isatine.
- antagonistes et inhibiteurs : Protéines virales.
- enzymologie : Virus du SRAS.
- pharmacologie : Chymotrypsine, Inhibiteurs de protéases, Isatine, Papaïne, Trypsine.
- synthèse chimique : Inhibiteurs de protéases, Isatine.
- Activation enzymatique, Cysteine endopeptidases, Endopeptidases, Humains, Inhibiteurs de protéases, Relation structure-activité, Simulation numérique, Sites de fixation, Spécificité du substrat, Structure moléculaire, Transfert d'énergie par résonance de fluorescence.
English descriptors
- KwdEn :
- Binding Sites, Chymotrypsin (pharmacology), Computer Simulation, Cysteine Endopeptidases, Endopeptidases, Enzyme Activation, Fluorescence Resonance Energy Transfer, Humans, Isatin (analogs & derivatives), Isatin (chemical synthesis), Isatin (pharmacology), Molecular Structure, Papain (pharmacology), Protease Inhibitors (chemical synthesis), Protease Inhibitors (chemistry), Protease Inhibitors (pharmacology), SARS Virus (enzymology), Structure-Activity Relationship, Substrate Specificity, Trypsin (pharmacology), Viral Proteins (antagonists & inhibitors).
- MESH :
- chemical , analogs & derivatives : Isatin.
- chemical , antagonists & inhibitors : Viral Proteins.
- chemical , chemical synthesis : Isatin, Protease Inhibitors.
- chemical , chemistry : Protease Inhibitors.
- chemical , pharmacology : Chymotrypsin, Isatin, Papain, Protease Inhibitors, Trypsin.
- enzymology : SARS Virus.
- Binding Sites, Computer Simulation, Cysteine Endopeptidases, Endopeptidases, Enzyme Activation, Fluorescence Resonance Energy Transfer, Humans, Molecular Structure, Structure-Activity Relationship, Substrate Specificity.
Abstract
N-Substituted isatin derivatives were prepared from the reaction of isatin and various bromides via two steps. Bioactivity assay results (in vitro tests) demonstrated that some of these compounds are potent and selective inhibitors against SARS coronavirus 3CL protease with IC50 values ranging from 0.95 to 17.50 microM. Additionally, isatin 4o exhibited more potent inhibition for SARS coronavirus protease than for other proteases including papain, chymotrypsin, and trypsin.
DOI: 10.1016/j.bmcl.2005.04.027
PubMed: 15896959
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pubmed:15896959Le document en format XML
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first="Shyh-Fong" last="Chen">Shyh-Fong Chen</name></author><author><name sortKey="Liu, Lee Tai" sort="Liu, Lee Tai" uniqKey="Liu L" first="Lee Tai" last="Liu">Lee Tai Liu</name></author><author><name sortKey="Wu, Ying Ta" sort="Wu, Ying Ta" uniqKey="Wu Y" first="Ying-Ta" last="Wu">Ying-Ta Wu</name></author><author><name sortKey="Kuo, Chih Jung" sort="Kuo, Chih Jung" uniqKey="Kuo C" first="Chih-Jung" last="Kuo">Chih-Jung Kuo</name></author><author><name sortKey="Chen, Tom Shieh Shung" sort="Chen, Tom Shieh Shung" uniqKey="Chen T" first="Tom Shieh-Shung" last="Chen">Tom Shieh-Shung Chen</name></author><author><name sortKey="Juang, Shin Hun" sort="Juang, Shin Hun" uniqKey="Juang S" first="Shin-Hun" last="Juang">Shin-Hun Juang</name></author></analytic><series><title level="j">Bioorganic & medicinal chemistry letters</title><idno type="ISSN">0960-894X</idno><imprint><date when="2005" 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Virus</term></keywords><keywords scheme="MESH" qualifier="pharmacologie" xml:lang="fr"><term>Chymotrypsine</term><term>Inhibiteurs de protéases</term><term>Isatine</term><term>Papaïne</term><term>Trypsine</term></keywords><keywords scheme="MESH" qualifier="synthèse chimique" xml:lang="fr"><term>Inhibiteurs de protéases</term><term>Isatine</term></keywords><keywords scheme="MESH" xml:lang="en"><term>Binding Sites</term><term>Computer Simulation</term><term>Cysteine Endopeptidases</term><term>Endopeptidases</term><term>Enzyme Activation</term><term>Fluorescence Resonance Energy Transfer</term><term>Humans</term><term>Molecular Structure</term><term>Structure-Activity Relationship</term><term>Substrate Specificity</term></keywords><keywords scheme="MESH" xml:lang="fr"><term>Activation enzymatique</term><term>Cysteine endopeptidases</term><term>Endopeptidases</term><term>Humains</term><term>Inhibiteurs de protéases</term><term>Relation structure-activité</term><term>Simulation 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Bioactivity assay results (in vitro tests) demonstrated that some of these compounds are potent and selective inhibitors against SARS coronavirus 3CL protease with IC50 values ranging from 0.95 to 17.50 microM. Additionally, isatin 4o exhibited more potent inhibition for SARS coronavirus protease than for other proteases including papain, chymotrypsin, and trypsin.</div></front></TEI></record>Pour manipuler ce document sous Unix (Dilib)
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