Abstract
Dinucleosides containing a thiazolidin-4-one linkage were prepared by one-pot tandem Staudinger/aza-Wittig/intermolecular cyclization under microwave irradiation and their structures were confirmed. Preliminary examination of HIV-RT inhibition showed that the dinucleosides containing (R)-thiazolidin-4-one linkage are significantly more active than those containing (S)-thiazolidin-4-one linkage.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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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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HIV Infections / drug therapy
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HIV Reverse Transcriptase / antagonists & inhibitors*
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HIV Reverse Transcriptase / metabolism
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HIV-1 / enzymology*
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Microwaves
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Models, Molecular
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Nucleosides / chemical synthesis
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Nucleosides / chemistry*
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Nucleosides / pharmacology
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Thiazolidines / chemical synthesis
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Thiazolidines / chemistry*
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Thiazolidines / pharmacology
Substances
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Enzyme Inhibitors
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Nucleosides
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Thiazolidines
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HIV Reverse Transcriptase