Recent progress in the medicinal chemistry of vancomycin

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    1 Citation (Scopus)


    The increasing incidence of vancomycin resistance in clinical settings has prompted research into new antibiotics against vancomycin-resistant strains. Recent efforts toward the development of novel glycopeptide antibiotics including our works are reviewed. Introduction of a carbon substituent at the amino acid residue 2 of vancomycin by Suzuki-Miyaura cross-coupling reaction led to an enhancement of antibacterial activity against vancomycin-resistant Staphylococcus aureus (VRSA). The potent activities of Van-M-02 against the Gram-positive bacteria including vancomycin-resistant enterococci (VRE) and VRSA are also described, and its mode of action was investigated with an assay system employing cell-membrane fraction of S.aureus as a crude enzyme mixture.

    Original languageEnglish
    Pages (from-to)480-489
    Number of pages10
    JournalYuki Gosei Kagaku Kyokaishi/Journal of Synthetic Organic Chemistry
    Issue number5
    Publication statusPublished - 2010 May


    • Antibiotics
    • Mode of action
    • S. aureus
    • Suzuki-miyaura cross-coupling
    • VRE
    • VRSA
    • Van-M-02
    • Vancomycin

    ASJC Scopus subject areas

    • Organic Chemistry


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