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  • Structurally optimized potent dual-targeting NBTI antibacterials with an enhanced bifurcated halogen-bonding propensity
    Kokot, Maja, 1995- ...
    We designed and synthesized an optimized library of novel bacterial topoisomerase inhibitors with p-halogenated phenyl right-hand side fragments and significantly enhanced and balanced dual-targeted ... DNA gyrase and topoisomerase IV activities of Staphylococcus aureus and Escherichia coli. By increasing the electron-withdrawing properties of the p-halogenated phenyl right-hand side fragment and maintaining a similar lipophilicity and size, an increased potency was achieved, indicating that the antibacterial activities of this series of novel bacterial topoisomerase inhibitors against all target enzymes are determined by halogen-bonding rather than van der Waals interactions. They show nanomolar enzyme inhibitory and whole-cell antibacterial activities against S. aureus and methicillin-resistant S. aureus (MRSA) strains. However, due to the relatively high substrate specificity for the bacterial efflux pumps, they tend to be less potent against E. coli and other Gram-negative pathogens.
    Vir: ACS Medicinal Chemistry Letters. - ISSN 1948-5875 (Vol. 12, iss. 9, 2021, str. 1478-1485)
    Vrsta gradiva - članek, sestavni del ; neleposlovje za odrasle
    Leto - 2021
    Jezik - angleški
    COBISS.SI-ID - 73185027

    Povezava(-e):

    https://pubs.acs.org/doi/10.1021/acsmedchemlett.1c00345
    https://pubs.acs.org/doi/pdf/10.1021/acsmedchemlett.1c00345
    Repozitorij Univerze v Ljubljani – RUL
    DOI

vir: ACS Medicinal Chemistry Letters. - ISSN 1948-5875 (Vol. 12, iss. 9, 2021, str. 1478-1485)
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