20.500.12556/RUL-140640 The structural features of novel bacterial topoisomerase inhibitors that define their activity on topoisomerase IV 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. genetics inhibition bacteria phenyls farmacevtska kemija bakterijska rezistenca true false true Angleški jezik Slovenski jezik Članek v reviji 2022-09-16 15:02:52 2022-09-16 15:02:56 2022-09-24 04:12:17 0000-00-00 00:00:00 2022 0 0 Str. 6431–6440 iss. 9 Vol. 65 2022 0000-00-00 Zaloznikova Objavljeno NiDoloceno 0000-00-00 0000-00-00 0000-00-00 615.4:54:615.015.8 0022-2623 10.1021/acs.jmedchem.2c00039 106691587 acs.jmedchem.2c00039_The_Structural_Features_of_Novel_Bacterial_Topoisomerase_Inhibitors_that_Define_Their_Activity_on_Topoisomerase_IV.pdf acs.jmedchem.2c00039_The_Structural_Features_of_Novel_Bacterial_Topoisomerase_Inhibitors_that_Define_Their_Activity_on_Topoisomerase_IV.pdf 1 E7BE7C5FBF565F032561CBA64E64B6A3 14d24003249a6b006efd27d0a1d22687eec2925e4102fef66322ea2c9ddd940d 48f837e6-3b28-11ed-9c94-00155dcfd717 https://repozitorij.uni-lj.si/Dokument.php?lang=slv&id=162061 https://pubs.acs.org/doi/10.1021/acs.jmedchem.2c00039 1 cfd07910-35bf-11ed-92af-00155dcfd717 https://repozitorij.uni-lj.si/Dokument.php?lang=slv&id=161429 Fakulteta za farmacijo 0 0 0