Abstract
Appropriately protected nucleoside 5'-O-(2-thio-1,3,2-dithiaphospholanes) react with inorganic pyrophosphate in the presence of a strong base catalyst (DBU) to give nucleoside 5'-O-(1,1-dithiotriphosphates) 1a-g. The latter compounds, including an AZT analogue, show modest antivirial activity against HIV-1 and HIV-2 replication in CEM cells. The AZT and deoxyadenosine derivatives were found to be inhibitors of HIV reverse transcriptase.
Publication types
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Research Support, U.S. Gov't, P.H.S.
MeSH terms
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Antiviral Agents / chemical synthesis*
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Antiviral Agents / pharmacology
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Cell Line
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HIV Reverse Transcriptase
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HIV-1 / drug effects
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HIV-1 / physiology
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HIV-2 / drug effects
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HIV-2 / physiology
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Reverse Transcriptase Inhibitors
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Thionucleotides / chemical synthesis*
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Thionucleotides / pharmacology
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Virus Replication / drug effects
Substances
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Antiviral Agents
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Reverse Transcriptase Inhibitors
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Thionucleotides
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HIV Reverse Transcriptase