Abstract
Novel 2-(coumarin-4-yloxy)-4,6-(substituted)-s-triazine derivatives i. e., diaryltriazine (DATA) are reported as novel non-nucleoside reverse transcriptase inhibitors (NNRTIs), were synthesized and their activities against human immunodeficiency virus HIV-1 (III-B), HIV-2 (ROD), and the double RT mutant HIV-1 (K103N and Y181C) were assessed. Modifications at positions 4 and 6 of the coumarinyl-triazine scaffold generated interesting derivatives displaying good to moderate anti-HIV activity against selected HIV strains as compared to nevirapine and efavirenz. The synthesized compounds were characterized by FTIR, (1)H-NMR, and mass spectral data together with elemental analysis.
MeSH terms
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4-Hydroxycoumarins / chemical synthesis*
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4-Hydroxycoumarins / chemistry
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4-Hydroxycoumarins / 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
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Drug Evaluation, Preclinical
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HIV Reverse Transcriptase / antagonists & inhibitors*
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HIV-1 / drug effects
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HIV-1 / enzymology
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HIV-2 / drug effects
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HIV-2 / enzymology
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Humans
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Magnetic Resonance Spectroscopy
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Mass Spectrometry
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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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Spectroscopy, Fourier Transform Infrared
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Structure-Activity Relationship
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Triazines / chemical synthesis*
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Triazines / chemistry
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Triazines / pharmacology
Substances
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4-Hydroxycoumarins
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Anti-HIV Agents
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Reverse Transcriptase Inhibitors
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Triazines
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HIV Reverse Transcriptase
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4-hydroxycoumarin