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  • New N-phenylpyrrolamide DNA gyrase B inhibitors : optimisation of efficacy and antibacterial activity
    Durcik, Martina ...
    The ATP binding site located on the subunit B of DNA gyrase is an attractive target for the development of new antibacterial agents. In recent decades, several small-molecule inhibitor classes have ... been discovered but none has so far reached the market. We present here the discovery of a promising new series of N-phenylpyrrolamides with low nanomolar IC50 values against DNA gyrase, and submicromolar IC50 values against topoisomerase IV from Escherichia coli and Staphylococcus aureus. The most potent compound in the series has an IC50 value of 13nM against E. coli gyrase. Minimum inhibitory concentrations (MICs) against Gram-positive bacteria are in the low micromolar range. The oxadiazolone derivative 11a, with an IC50 value of 85nM against E. coli DNA gyrase displays the most potent antibacterial activity, with MIC values of 1.56 microM against Enterococcus faecalis, and 3.13 microM against wild type S. aureus, methicillin-resistant S. aureus (MRSA) and vancomycin-resistant Enterococcus (VRE). The activity against wild type E. coli in the presence of efflux pump inhibitor phenylalanine-arginine beta-naphthylamide (PA(beta)N) is 4.6microM.
    Source: European journal of medicinal chemistry. - ISSN 0223-5234 (Vol. 154, June 2018, str. 117-132)
    Type of material - article, component part ; adult, serious
    Publish date - 2018
    Language - english
    COBISS.SI-ID - 4504945

    Link(s):

    https://www.sciencedirect.com/science/article/pii/S022352341830415X

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