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  • Dual Escherichia coli DNA gyrase A and B inhibitors with antibacterial activity [Elektronski vir]
    Fois, Benedetta ...
    The emergence of multidrug resistant bacteria is a global health threat necessitating the discovery of new antibacterials and novel strategies for fighting bacterial infections. We report ... first-in-class DNA gyrase B (GyrB) inhibitor/ciprofloxacin hybrids that display antibacterial activity against Escherichia coli. Whereas DNA gyrase ATPase inhibition experiments, DNA gyrase supercoiling assays, and in-vitro antibacterial assays suggest binding of the hybrids to the E. coli GyrA and GyrB subunits, an interaction with the GyrA fluoroquinolone-binding site seems to be solely responsible for their antibacterial activity. Our results provide a foundation for a new concept of facilitating entry of nonpermeating GyrB inhibitors into bacteria by conjugation with ciprofloxacin, a highly permeable GyrA inhibitor. A hybrid molecule containing GyrA and GyrB inhibitor parts entering the bacterial cell would then elicit a strong antibacterial effect by inhibition of both the GyrA and GyrB subunits of DNA gyrase and potentially slow bacterial resistance development.
    Source: ChemMedChem. - ISSN 1860-7187 (Vol. 15, iss. 3, 2020, str. 265-269)
    Type of material - e-article
    Publish date - 2020
    Language - english
    COBISS.SI-ID - 4865393

    Link(s):

    https://onlinelibrary.wiley.com/doi/abs/10.1002/cmdc.201900607

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