Abstract
4-(Arylthio)-pyridin-2(1H)-ones variously substituted in their 3-, 5-, and 6-positions have been synthesized as a new series of 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine (HEPT)-pyridinone hybrid molecules. Biological studies revealed that some of them show potent HIV-1 specific reverse transcriptase inhibitory properties. Compounds 16 and 7c, the most active ones, inhibit the replication of HIV-1 at 3 and 6 nM, respectively.
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 / pharmacology
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HIV Reverse Transcriptase
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HIV-1 / drug effects
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HIV-1 / enzymology*
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HIV-1 / physiology
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HIV-2 / enzymology
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Kinetics
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Molecular Structure
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Pyridones / chemical synthesis*
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Pyridones / pharmacology
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RNA-Directed DNA Polymerase / metabolism*
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Recombinant Proteins / antagonists & inhibitors
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Reverse Transcriptase Inhibitors / chemical synthesis*
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Reverse Transcriptase Inhibitors / pharmacology
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Structure-Activity Relationship
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Virus Replication / drug effects
Substances
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3-amino-5-ethyl-6-methyl-4-((3',5'-dimethylphenyl)thio)pyridin-2(1H)-one
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5-ethyl-6-methyl-3-nitro-4-((3',5'-dimethylphenyl)thio)pyridin-2(1H)-one
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Antiviral Agents
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Pyridones
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Recombinant Proteins
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Reverse Transcriptase Inhibitors
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HIV Reverse Transcriptase
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RNA-Directed DNA Polymerase