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.
Publication types
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Research Support, N.I.H., Extramural
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Research Support, Non-U.S. Gov't
MeSH terms
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Amino Acid Sequence
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Antiviral Agents / chemical synthesis*
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Antiviral Agents / chemistry
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Antiviral Agents / pharmacology
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Benzothiazoles / chemical synthesis
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Benzothiazoles / chemistry
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Benzothiazoles / pharmacology
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Chymases / antagonists & inhibitors
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Chymases / metabolism
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Computer Simulation
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Coronavirus 3C Proteases
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Cysteine Endopeptidases / metabolism
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Drug Design
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Ketones / chemical synthesis
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Ketones / chemistry
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Peptides / chemical synthesis
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Peptides / chemistry
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Peptides / pharmacology
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Protease Inhibitors / chemical synthesis*
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Protease Inhibitors / chemistry
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Protease Inhibitors / pharmacology
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Pyrrolidinones / chemical synthesis
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Pyrrolidinones / chemistry
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Pyrrolidinones / pharmacology
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Severe acute respiratory syndrome-related coronavirus*
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Structure-Activity Relationship
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Thiazoles / chemical synthesis
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Thiazoles / chemistry
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Thiazoles / pharmacology
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Viral Proteins / antagonists & inhibitors*
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Viral Proteins / metabolism
Substances
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Antiviral Agents
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Benzothiazoles
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Ketones
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Peptides
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Protease Inhibitors
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Pyrrolidinones
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Thiazoles
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Viral Proteins
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Chymases
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Cysteine Endopeptidases
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Coronavirus 3C Proteases