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  • Benzothiazole DNA gyrase inhibitors and their conjugates with siderophore mimics : design, synthesis and evaluation
    Durcik, Martina ...
    Benzothiazole-based bacterial DNA gyrase and topoisomerase IV inhibitors are promising new antibacterial agents with potent activity against Gram-positive and Gram-negative bacterial strains. The aim ... of this study was to improve the uptake of these inhibitors into the cytoplasm of Gram-negative bacteria by conjugating them to the small siderophore mimics. The best conjugate 18b displayed potent Escherichia coli DNA gyrase and topoisomerase IV inhibition. The interaction analysis of molecular dynamics simulation trajectory showed the important contribution of the siderophore mimic moiety to binding affinity. By NMR spectroscopy, we demonstrated that the hydroxypyridinone moiety alone was responsible for the chelation of iron(III). Moreover, 18b showed an enhancement of antibacterial activity against E. coli JW5503 in an iron-depleted medium, clearly indicating an increased uptake of 18b in this bacterial strain.
    Source: RSC advances [Elektronski vir]. - ISSN 2046-2069 (Vol. 14, iss. 5, 2024, str. 2905-2917)
    Type of material - e-article ; adult, serious
    Publish date - 2024
    Language - english
    COBISS.SI-ID - 181568259

    Link(s):

    https://pubs.rsc.org/en/content/articlelanding/2024/ra/d3ra08337c
    DOI

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