Abstract
The synthesis and anti-HIV activity evaluation of a new series of 2,4-pyrimidinediones bearing a 6-(1-naphthoyl) group are described. In general, it was found that most of the title compounds showed good activities against human immunodeficiency virus type-1 (HIV-1). In particular, compound 26 displayed the most potent anti-HIV-1 activity (IC(50)=0.11+/-0.05 microM), inhibiting HIV-1 replication in MT-4 cells more effectively than HEPT (by 45-fold) and DDI (by 50-fold).
MeSH terms
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Alkenes / chemical synthesis*
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Alkenes / pharmacology
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Alkynes / chemical synthesis*
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Alkynes / pharmacology
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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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Cell Line, Tumor
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HIV Reverse Transcriptase / metabolism*
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HIV-1 / drug effects
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Humans
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Naphthalenes / chemical synthesis*
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Naphthalenes / pharmacology
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Reverse Transcriptase Inhibitors / chemical synthesis*
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Reverse Transcriptase Inhibitors / chemistry
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Reverse Transcriptase Inhibitors / pharmacology
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Uracil / analogs & derivatives*
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Uracil / chemical synthesis*
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Uracil / pharmacology
Substances
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Alkenes
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Alkynes
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Anti-HIV Agents
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Naphthalenes
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Reverse Transcriptase Inhibitors
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Uracil
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HIV Reverse Transcriptase