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A fine-tuned lipophilicity/hydrophilicity ratio governs antibacterial potency and selectivity of bifurcated halogen bond-forming NBTIs [Elektronski vir]Kolarič, Anja, farmacevtka ...Herein, we report the design of a focused library of novel bacterial topoisomerase inhibitors (NBTIs) based on innovative mainly monocyclic right-hand side fragments active against DNA gyrase and ... Topo IV. They exhibit a very potent and wide range of antibacterial activity, even against some of the most concerning hard-to-treat pathogens for which new antibacterials are urgently needed, as reported by the WHO and CDC. NBTIs enzyme activity and whole cell potency seems to depend on the fine-tuned lipophilicity/hydrophilicity ratio that governs the permeability of those compounds through the bacterial membranes. Lipophilicity of NBTIs is apparently optimal for passing through the membrane of Gram-positive bacteria, but the higher, although not excessive lipophilicity and suitable hydrophilicity seems to determine the passage through Gram-negative bacterial membranes. However, due to the considerable hERG inhibition, which is still at least two orders of magnitude away from MICs, continued optimization is required to realize their full potential.Source: Antibiotics [Elektronski vir]. - ISSN 2079-6382 (Vol. 10, no. 7, art. 862, 2021, 30 str.)Type of material - e-article ; adult, seriousPublish date - 2021Language - englishCOBISS.SI-ID - 70416899
Author
Kolarič, Anja, farmacevtka |
Kokot, Maja, 1995- |
Hrast, Martina |
Weiss, Matjaž |
Zdovc, Irena |
Trontelj, Jurij |
Žakelj, Simon |
Anderluh, Marko |
Minovski, Nikola
Topics
Farmacevtska kemija |
antibacterials |
drug discovery |
DNA gyrase inhibitors |
topoisomerase IV inhibitors |
intercalators |
novel bacterial topoisomerase inhibitors |
antibakterijska sredstva |
raziskave zdravil |
zaviralci DNA giraz |
zaviralci topoizomeraze IV |
interkalator |
novi zaviralci bakterijske topoizomeraze
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Author | Kolarič, Anja, farmacevtka ... |
Title | A fine-tuned lipophilicity/hydrophilicity ratio governs antibacterial potency and selectivity of bifurcated halogen bond-forming NBTIs [Elektronski vir] |
Publication date | 2021-07-15 |
COBISS.SI-ID | 70416899 |
Publication version in repository | Publisher's version |
Publication licence | Creative Commons Attribution 4.0 International |
Embargo | Immediate publication for public |
Project(s) from which the publication was funded
Title | Acronym | Project ID | Funder |
---|---|---|---|
Modeliranje kemijskih procesov in lastnosti spojin | P1-0017-2020 |
Javna agencija za znanstvenoraziskovalno in inovacijsko dejavnost Republike Slovenije |
|
Farmacevtska kemija: načrtovanje, sinteza in vrednotenje učinkovin | P1-0208-2015 |
Javna agencija za znanstvenoraziskovalno in inovacijsko dejavnost Republike Slovenije |
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Database name | Field | Year |
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Links to authors' personal bibliographies | Links to information on researchers in the SICRIS system |
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Kolarič, Anja, farmacevtka | 38261 |
Kokot, Maja, 1995- | 53608 |
Hrast, Martina | 32036 |
Weiss, Matjaž | 50503 |
Zdovc, Irena | 12682 |
Trontelj, Jurij | 23420 |
Žakelj, Simon | 22659 |
Anderluh, Marko | 21456 |
Minovski, Nikola | 29497 |
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