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  • Title: The synthesis and antistaphylococcal activity of 9, 13-disubstituted berberine derivatives.
    Author: Wang J, Yang T, Chen H, Xu YN, Yu LF, Liu T, Tang J, Yi Z, Yang CG, Xue W, Yang F.
    Journal: Eur J Med Chem; 2017 Feb 15; 127():424-433. PubMed ID: 28092858.
    Abstract:
    A series of novel 9, 13-disubstituted berberine derivatives have been synthesized and evaluated for the antibacterial activities against Staphylococcus aureus, including Newman strain and multidrug-resistant strains (NRS-1, NRS-70, NRS-100, NRS-108, and NRS-271). Compound 20 shows the most potent activity against the growth of Newman strain, with a MIC value of 0.78 μg/mL, which is comparable with the positive control vancomycin. In addition, compound 20, 21, and 33 are highly antistaphylococcal active against five strains of multidrug-resistant S. aureus, with MIC values of 0.78-1.56 μg/mL. Of note, theses antibacterial active compounds have no obvious toxicity to the viability of human fibroblast (HAF) cells at the MIC concentration.
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