New developments for the design, synthesis and biological evaluation of potent SARS-CoV 3CL(pro) inhibitors.
Identifieur interne : 001930 ( PubMed/Corpus ); précédent : 001929; suivant : 001931New developments for the design, synthesis and biological evaluation of potent SARS-CoV 3CL(pro) inhibitors.
Auteurs : Thomas Regnier ; Diganta Sarma ; Koushi Hidaka ; Usman Bacha ; Ernesto Freire ; Yoshio Hayashi ; Yoshiaki KisoSource :
- Bioorganic & medicinal chemistry letters [ 1464-3405 ] ; 2009.
English descriptors
- KwdEn :
- Amino Acid Sequence, Antiviral Agents (chemical synthesis), Antiviral Agents (chemistry), Antiviral Agents (pharmacology), Benzothiazoles (chemical synthesis), Benzothiazoles (chemistry), Benzothiazoles (pharmacology), Chymases (antagonists & inhibitors), Chymases (metabolism), Computer Simulation, Cysteine Endopeptidases (metabolism), Drug Design, Ketones (chemical synthesis), Ketones (chemistry), Peptides (chemical synthesis), Peptides (chemistry), Peptides (pharmacology), Protease Inhibitors (chemical synthesis), Protease Inhibitors (chemistry), Protease Inhibitors (pharmacology), Pyrrolidinones (chemical synthesis), Pyrrolidinones (chemistry), Pyrrolidinones (pharmacology), SARS Virus, Structure-Activity Relationship, Thiazoles (chemical synthesis), Thiazoles (chemistry), Thiazoles (pharmacology), Viral Proteins (antagonists & inhibitors), Viral Proteins (metabolism).
- MESH :
- chemical , antagonists & inhibitors : Chymases, Viral Proteins.
- chemical , chemical synthesis : Antiviral Agents, Benzothiazoles, Ketones, Peptides, Protease Inhibitors, Pyrrolidinones, Thiazoles.
- chemical , chemistry : Antiviral Agents, Benzothiazoles, Ketones, Peptides, Protease Inhibitors, Pyrrolidinones, Thiazoles.
- chemical , metabolism : Chymases, Cysteine Endopeptidases, Viral Proteins.
- chemical , pharmacology : Antiviral Agents, Benzothiazoles, Peptides, Protease Inhibitors, Pyrrolidinones, Thiazoles.
- Amino Acid Sequence, Computer Simulation, Drug Design, SARS Virus, Structure-Activity Relationship.
Abstract
A series of trifluoromethyl, benzothiazolyl or thiazolyl ketone-containing peptidic compounds as SARS-CoV 3CL protease inhibitors were developed and their potency was evaluated by in vitro protease inhibitory assays. Three candidates had encouraging results for the development of new anti-SARS compounds.
DOI: 10.1016/j.bmcl.2009.03.118
PubMed: 19362479
Links to Exploration step
pubmed:19362479Le document en format XML
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<term>Cysteine Endopeptidases (metabolism)</term>
<term>Drug Design</term>
<term>Ketones (chemical synthesis)</term>
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<term>Peptides (chemical synthesis)</term>
<term>Peptides (chemistry)</term>
<term>Peptides (pharmacology)</term>
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<term>Protease Inhibitors (chemistry)</term>
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<front><div type="abstract" xml:lang="en">A series of trifluoromethyl, benzothiazolyl or thiazolyl ketone-containing peptidic compounds as SARS-CoV 3CL protease inhibitors were developed and their potency was evaluated by in vitro protease inhibitory assays. Three candidates had encouraging results for the development of new anti-SARS compounds.</div>
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