Abstract
In an attempt to combine the HIV-inhibitory capacity of different 2',3'-dideoxynucleoside (ddN) analogs, we have designed and synthesized several dimers of [AZT]-[AZT] and [AZT]-[d4T]. In addition, we also synthesized the dimers of 1-(1H-benzimidazol-1-yl)-1-deoxy-beta-D-ribofuranose. The in vitro anti-HIV activity of these compounds on a pseudotype virus, pNL4-3.Luc.R-E-, in the 293T cells has been determined. Among these compounds, 2,2'-(propane-1,3-diyl)bis[1-(beta-D-ribofuranosyl)-1H-benzimidazole] showed the highest anti-HIV activity with similar effect as AZT.
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 / chemistry
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Anti-HIV Agents / pharmacology
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Benzimidazoles / chemical synthesis*
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Benzimidazoles / chemistry*
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Benzimidazoles / pharmacology
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Cell Line
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Dideoxynucleosides / chemical synthesis
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Dideoxynucleosides / chemistry*
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Dideoxynucleosides / pharmacology
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Dimerization
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HIV Core Protein p24 / metabolism
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Humans
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Nucleosides / chemical synthesis*
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Nucleosides / chemistry
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Nucleosides / pharmacology
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Zidovudine / chemistry
Substances
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2,2'-(propane-1,3-diyl)bis(1-(ribofuranosyl)-1H-benzimidazole)
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Anti-HIV Agents
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Benzimidazoles
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Dideoxynucleosides
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HIV Core Protein p24
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Nucleosides
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Zidovudine
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benzimidazole