Synthesis and evaluation of isatin derivatives as effective SARS coronavirus 3CL protease inhibitors.
Identifieur interne : 002736 ( PubMed/Curation ); précédent : 002735; suivant : 002737Synthesis 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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<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>
</front>
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<Abstract><AbstractText>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.</AbstractText>
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<AuthorList CompleteYN="Y"><Author ValidYN="Y"><LastName>Chen</LastName>
<ForeName>Li-Rung</ForeName>
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<AffiliationInfo><Affiliation>Development Center for Biotechnology, 102, Lane 169, Kang Ning St., Xi Zhi 221, Taipei, Taiwan, ROC.</Affiliation>
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