Abstract
Aryl diketoacids have been identified as the first SARS-CoV NTPase/helicase inhibitors with a distinct pharmacophore featuring an arylmethyl group attached to a diketoacid. In order to search for the pharmacophore space around the diketoacid core, three classes of dihydroxychromone derivatives were prepared. Based on SAR study, an extended feature of the pharmacophore model of SARS-CoV NTPase/helicase was proposed which is constituted of a diketoacid core, a hydrophobic arylmethyl substituent, and a free catechol unit.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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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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Catechols / chemistry
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Chromones / chemical synthesis
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Chromones / chemistry*
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Chromones / pharmacology
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DNA Helicases / antagonists & inhibitors*
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DNA Helicases / metabolism
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Enzyme Inhibitors / chemical synthesis
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Enzyme Inhibitors / chemistry*
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Enzyme Inhibitors / pharmacology
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Severe acute respiratory syndrome-related coronavirus / enzymology*
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Structure-Activity Relationship
Substances
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Antiviral Agents
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Catechols
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Chromones
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Enzyme Inhibitors
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DNA Helicases
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catechol