Design and synthesis of cinanserin analogs as severe acute respiratory syndrome coronavirus 3CL protease inhibitors.
Identifieur interne : 003133 ( Main/Exploration ); précédent : 003132; suivant : 003134Design and synthesis of cinanserin analogs as severe acute respiratory syndrome coronavirus 3CL protease inhibitors.
Auteurs : Qingang Yang [République populaire de Chine] ; Lili Chen ; Xuchang He ; Zhenting Gao ; Xu Shen ; Donglu BaiSource :
- Chemical & pharmaceutical bulletin [ 0009-2363 ] ; 2008.
Descripteurs français
- KwdFr :
- Antisérotonines (pharmacologie), Antisérotonines (synthèse chimique), Antiviraux (pharmacologie), Antiviraux (synthèse chimique), Cinansérine (analogues et dérivés), Cinansérine (pharmacologie), Cinansérine (synthèse chimique), Conception de médicament, Cysteine endopeptidases, Indicateurs et réactifs, Inhibiteurs de protéases (pharmacologie), Inhibiteurs de protéases (synthèse chimique), Modèles moléculaires, Protéines virales (antagonistes et inhibiteurs), Relation structure-activité, Spectrophotométrie IR, Spectroscopie par résonance magnétique, Transfert d'énergie par résonance de fluorescence, Virus du SRAS (enzymologie).
- MESH :
- analogues et dérivés : Cinansérine.
- antagonistes et inhibiteurs : Protéines virales.
- enzymologie : Virus du SRAS.
- pharmacologie : Antisérotonines, Antiviraux, Cinansérine, Inhibiteurs de protéases.
- synthèse chimique : Antisérotonines, Antiviraux, Cinansérine, Inhibiteurs de protéases.
- Conception de médicament, Cysteine endopeptidases, Indicateurs et réactifs, Modèles moléculaires, Relation structure-activité, Spectrophotométrie IR, Spectroscopie par résonance magnétique, Transfert d'énergie par résonance de fluorescence.
English descriptors
- KwdEn :
- Antiviral Agents (chemical synthesis), Antiviral Agents (pharmacology), Cinanserin (analogs & derivatives), Cinanserin (chemical synthesis), Cinanserin (pharmacology), Cysteine Endopeptidases, Drug Design, Fluorescence Resonance Energy Transfer, Indicators and Reagents, Magnetic Resonance Spectroscopy, Models, Molecular, Protease Inhibitors (chemical synthesis), Protease Inhibitors (pharmacology), SARS Virus (enzymology), Serotonin Antagonists (chemical synthesis), Serotonin Antagonists (pharmacology), Spectrophotometry, Infrared, Structure-Activity Relationship, Viral Proteins (antagonists & inhibitors).
- MESH :
- chemical , analogs & derivatives : Cinanserin.
- chemical , antagonists & inhibitors : Viral Proteins.
- chemical , chemical synthesis : Antiviral Agents, Cinanserin, Protease Inhibitors, Serotonin Antagonists.
- chemical , pharmacology : Antiviral Agents, Cinanserin, Protease Inhibitors, Serotonin Antagonists.
- chemical : Cysteine Endopeptidases, Indicators and Reagents.
- enzymology : SARS Virus.
- Drug Design, Fluorescence Resonance Energy Transfer, Magnetic Resonance Spectroscopy, Models, Molecular, Spectrophotometry, Infrared, Structure-Activity Relationship.
Abstract
The severe acute respiratory syndrome (SARS) coronavirus 3CL protease is an attractive target for the development of anti-SARS drugs. In this paper, cinanserin (1) analogs were synthesized and tested for the inhibitory activities against SARS-coronavirus (CoV) 3CL protease by fluorescence resonance energy transfer (FRET) assay. Four analogs show significant activities, especially compound 26 with an IC(50) of 1.06 microM.
DOI: 10.1248/cpb.56.1400
PubMed: 18827378
Affiliations:
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Le document en format XML
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Virus</term></keywords><keywords scheme="MESH" qualifier="pharmacologie" xml:lang="fr"><term>Antisérotonines</term><term>Antiviraux</term><term>Cinansérine</term><term>Inhibiteurs de protéases</term></keywords><keywords scheme="MESH" qualifier="synthèse chimique" xml:lang="fr"><term>Antisérotonines</term><term>Antiviraux</term><term>Cinansérine</term><term>Inhibiteurs de protéases</term></keywords><keywords scheme="MESH" xml:lang="en"><term>Drug Design</term><term>Fluorescence Resonance Energy Transfer</term><term>Magnetic Resonance Spectroscopy</term><term>Models, Molecular</term><term>Spectrophotometry, Infrared</term><term>Structure-Activity Relationship</term></keywords><keywords scheme="MESH" xml:lang="fr"><term>Conception de médicament</term><term>Cysteine endopeptidases</term><term>Indicateurs et réactifs</term><term>Modèles moléculaires</term><term>Relation structure-activité</term><term>Spectrophotométrie IR</term><term>Spectroscopie par résonance magnétique</term><term>Transfert d'énergie par résonance de fluorescence</term></keywords></textClass></profileDesc></teiHeader><front><div type="abstract" xml:lang="en">The severe acute respiratory syndrome (SARS) coronavirus 3CL protease is an attractive target for the development of anti-SARS drugs. In this paper, cinanserin (1) analogs were synthesized and tested for the inhibitory activities against SARS-coronavirus (CoV) 3CL protease by fluorescence resonance energy transfer (FRET) assay. Four analogs show significant activities, especially compound 26 with an IC(50) of 1.06 microM.</div></front></TEI><affiliations><list><country><li>République populaire de Chine</li></country></list><tree><noCountry><name sortKey="Bai, Donglu" sort="Bai, Donglu" uniqKey="Bai D" first="Donglu" last="Bai">Donglu Bai</name><name sortKey="Chen, Lili" sort="Chen, Lili" uniqKey="Chen L" first="Lili" last="Chen">Lili Chen</name><name sortKey="Gao, Zhenting" sort="Gao, Zhenting" uniqKey="Gao Z" first="Zhenting" last="Gao">Zhenting Gao</name><name sortKey="He, Xuchang" sort="He, Xuchang" uniqKey="He X" first="Xuchang" last="He">Xuchang He</name><name sortKey="Shen, Xu" sort="Shen, Xu" uniqKey="Shen X" first="Xu" last="Shen">Xu Shen</name></noCountry><country name="République populaire de Chine"><noRegion><name sortKey="Yang, Qingang" sort="Yang, Qingang" uniqKey="Yang Q" first="Qingang" last="Yang">Qingang Yang</name></noRegion></country></tree></affiliations></record>Pour manipuler ce document sous Unix (Dilib)
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