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  • The structural features of novel bacterial topoisomerase inhibitors that define their activity on topoisomerase IV
    Kokot, Maja, 1995- ...
    The continued emergence of bacterial resistance has created an urgent need for new and effective antibacterial agents. Bacterial type II topoisomerases, such as DNA gyrase and topoisomerase IV ... (topoIV), are well-validated targets for antibacterial chemotherapy. The novel bacterial topoisomerase inhibitors (NBTIs) represent one of the new promising classes of antibacterial agents. They can inhibit both of these bacterial targets; however, their potencies differ on the targets among species, making topoIV probably a primary target of NBTIs in Gram-negative bacteria. Therefore, it is important to gain an insight into the NBTIs key structural features that govern the topoIV inhibition. However, in Gram-positive bacteria, topoIV is also a significant target for achieving dual-targeting, which in turn contributes to avoiding bacterial resistance caused by single-target mutations. In this perspective, we address the structure–activity relationship guidelines for NBTIs that target the topoIV enzyme in Gram-positive and Gram-negative bacteria.
    Vir: Journal of medicinal chemistry. - ISSN 0022-2623 (Vol. 65, iss. 9, 2022, str. 6431–6440)
    Vrsta gradiva - članek, sestavni del ; neleposlovje za odrasle
    Leto - 2022
    Jezik - angleški
    COBISS.SI-ID - 106691587

    Povezava(-e):

    https://pubs.acs.org/doi/10.1021/acs.jmedchem.2c00039
    Repozitorij Univerze v Ljubljani – RUL
    DOI

vir: Journal of medicinal chemistry. - ISSN 0022-2623 (Vol. 65, iss. 9, 2022, str. 6431–6440)
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