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  • Synthesis and evaluation of N-phenylpyrrolamides as DNA gyrase B inhibitors [Elektronski vir]
    Durcik, Martina ...
    ATP-competitive inhibitors of DNA gyrase and topoisomerase IV are among the most interesting classes of antibacterial drugs that are unrepresented in the antibacterial pipeline. We developed 32 new ... N-phenylpyrrolamides and evaluated them against DNA gyrase and topoisomerase IV from E. coli and Staphylococcus aureus. Antibacterial activities were studied against Gram-positive and Gram-negative bacterial strains. The most potent compound displayed an IC50 of 47micro nm against E.coli DNA gyrase, and a minimum inhibitory concentration (MIC) of 12.5 microm against the Gram-positive Enterococcus faecalis. Some compounds displayed good antibacterial activities against an efflux-pump-deficient E. coli strain (MIC=6.25 microm) and against wild-type E. coli in the presence of efflux pump inhibitor PAbetaN (MIC=3.13 microm). Here we describe new findings regarding the structure-activity relationships of N-phenylpyrrolamide DNA gyrase B inhibitors and investigate the factors that are important for the antibacterial activity of this class of compounds.
    Source: ChemMedChem. - ISSN 1860-7187 (Vol. 13, iss. 2, 2018, str. 186-198)
    Type of material - e-article
    Publish date - 2018
    Language - english
    COBISS.SI-ID - 4461681

    Link(s):

    https://onlinelibrary.wiley.com/doi/10.1002/cmdc.201700549
    https://onlinelibrary.wiley.com/doi/epdf/10.1002/cmdc.201700549
    Repository of the University of Ljubljana – RUL
    DOI

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