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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<affiliation wicri:level="1"><nlm:affiliation>Development Center for Biotechnology, 102, Lane 169, Kang Ning St., Xi Zhi 221, Taipei, Taiwan, ROC.</nlm:affiliation>
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<author><name sortKey="Wang, Yu Chin" sort="Wang, Yu Chin" uniqKey="Wang Y" first="Yu-Chin" last="Wang">Yu-Chin Wang</name>
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<author><name sortKey="Chen, Shyh Fong" sort="Chen, Shyh Fong" uniqKey="Chen S" first="Shyh-Fong" last="Chen">Shyh-Fong Chen</name>
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<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>Isatin (analogs & derivatives)</term>
<term>Isatin (chemical synthesis)</term>
<term>Isatin (pharmacology)</term>
<term>Molecular Structure</term>
<term>Papain (pharmacology)</term>
<term>Protease Inhibitors (chemical synthesis)</term>
<term>Protease Inhibitors (chemistry)</term>
<term>Protease Inhibitors (pharmacology)</term>
<term>SARS Virus (enzymology)</term>
<term>Structure-Activity Relationship</term>
<term>Substrate Specificity</term>
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<term>Viral Proteins (antagonists & inhibitors)</term>
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<term>Chymotrypsine (pharmacologie)</term>
<term>Cysteine endopeptidases</term>
<term>Endopeptidases</term>
<term>Humains</term>
<term>Inhibiteurs de protéases ()</term>
<term>Inhibiteurs de protéases (pharmacologie)</term>
<term>Inhibiteurs de protéases (synthèse chimique)</term>
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<term>Protéines virales (antagonistes et inhibiteurs)</term>
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<term>Spécificité du substrat</term>
<term>Structure moléculaire</term>
<term>Transfert d'énergie par résonance de fluorescence</term>
<term>Trypsine (pharmacologie)</term>
<term>Virus du SRAS (enzymologie)</term>
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<keywords scheme="MESH" type="chemical" qualifier="chemical synthesis" xml:lang="en"><term>Isatin</term>
<term>Protease Inhibitors</term>
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<term>Isatin</term>
<term>Papain</term>
<term>Protease Inhibitors</term>
<term>Trypsin</term>
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<keywords scheme="MESH" qualifier="analogues et dérivés" xml:lang="fr"><term>Isatine</term>
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<keywords scheme="MESH" qualifier="enzymologie" xml:lang="fr"><term>Virus du SRAS</term>
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<term>Inhibiteurs de protéases</term>
<term>Isatine</term>
<term>Papaïne</term>
<term>Trypsine</term>
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<term>Isatine</term>
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<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>
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<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 numérique</term>
<term>Sites de fixation</term>
<term>Spécificité du substrat</term>
<term>Structure moléculaire</term>
<term>Transfert d'énergie par résonance de fluorescence</term>
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<front><div type="abstract" xml:lang="en">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.</div>
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