Abstract
The first TSAO derivative that lacks the amino group at the 3'-spiro moiety has been prepared. This molecule retained its HIV-1 specificity (NNRTI characteristic) but did not select for any of the classical NNRTI-specific mutations in the NNRTI binding pocket, including 138-Lys (TSAO resistant strain).
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Anti-HIV Agents / chemical synthesis*
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Anti-HIV Agents / pharmacology
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Deamination
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HIV Reverse Transcriptase / antagonists & inhibitors
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HIV Reverse Transcriptase / genetics
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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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Humans
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Mutation
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Reverse Transcriptase Inhibitors / chemical synthesis*
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Reverse Transcriptase Inhibitors / pharmacology
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Spiro Compounds / chemistry*
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Spiro Compounds / pharmacology
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Substrate Specificity
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Thymidine / analogs & derivatives*
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Thymidine / chemistry*
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Thymidine / pharmacology
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Uridine / analogs & derivatives
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Virus Replication / drug effects
Substances
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Anti-HIV Agents
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Reverse Transcriptase Inhibitors
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Spiro Compounds
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HIV Reverse Transcriptase
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Thymidine
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TSAO-T
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Uridine