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Synthesis, characterization, molecular docking and anti-tubercular activity of Plumbagin-Isoniazid Analog and its β-cyclodextrin conjugate.

Bioorganic & Medicinal Chemistry Letters(2014)

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摘要
A novel Plumbagin–Isoniazid Analog (PLIHZ) and its β-cyclodextrin inclusion complex (PLIHZCD) is prepared, characterized and evaluated for antitubercular activity under low and high iron conditions. PLIHZCD exhibited superior activity PLIHZ and PL under 7H9 medium conditions. The standard compound INH exhibited higher MIC values under low iron conditions, whereas it’s note-worthy that the new conjugate PLIHZ exhibited potent MIC value than INH under similar conditions indicating the advantage of combining plumbagin with INH to overcome INH resistance.
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关键词
Plumbagin,Plumbagin–Isoniazid Analog,β-Cyclodextrin,Inclusion complex,Antitubercular activity,Molecular docking
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