Abstract
Glycyrrhizin (GL) was shown to inhibit SARS-coronavirus (SARS-CoV) replication in vitro. Here the anti-SARS-CoV activity of 15 GL derivatives was tested. The introduction of 2-acetamido-beta-d-glucopyranosylamine into the glycoside chain of GL resulted in 10-fold increased anti-SARS-CoV activity compared to GL. Amides of GL and conjugates of GL with two amino acid residues and a free 30-COOH function presented up to 70-fold increased activity against SARS-CoV but also increased cytotoxicity resulting in decreased selectivity index.
MeSH terms
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Animals
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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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Chlorocebus aethiops
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Glycyrrhizic Acid / analogs & derivatives*
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Glycyrrhizic Acid / chemical synthesis*
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Glycyrrhizic Acid / chemistry
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Glycyrrhizic Acid / pharmacology
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Severe acute respiratory syndrome-related coronavirus / drug effects*
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Severe acute respiratory syndrome-related coronavirus / isolation & purification
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Structure-Activity Relationship
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Vero Cells
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Virus Replication / drug effects
Substances
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Antiviral Agents
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Glycyrrhizic Acid