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Diminishing hERG inhibitory activity of aminopiperidine-naphthyridine linked NBTI antibacterials by structural and physicochemical optimizationsKokot, Maja, 1995- ...Novel bacterial topoisomerase inhibitors (NBTIs) are an important new class of antibacterials targeting bacterial type II topoisomerases (DNA gyrase and topoisomerase IV). Notwithstanding their ... potent antibacterial activity, they suffer from a detrimental class-related hERG blockage. In this study, we designed and synthesized an optimized library of NBTIs comprising different linker moieties that exhibit reduced hERG inhibition and retain inhibitory potencies on DNA gyrase and topoisomerase IV of Staphylococcus aureus and Escherichia coli, respectively, as well as potent antibacterial activities. Substitution of the linker’s tertiary amine with polar groups outcome in diminished hERG inhibition. Compound 17 expresses nanomolar enzyme inhibitory potency and antibacterial activity against both Gram-positive and Gram-negative bacteria as well as reduced hERG inhibition relative to our previously published NBTI analogs. Here, we point to some important NBTI’s structural features that influence their hERG inhibitory activity.Source: Bioorganic chemistry. - ISSN 0045-2068 (Vol. 128, 2022, 14 str.)Type of material - article, component part ; adult, seriousPublish date - 2022Language - englishCOBISS.SI-ID - 118137091
Author
Kokot, Maja, 1995- |
Weiss, Matjaž |
Zdovc, Irena |
Anderluh, Marko |
Hrast, Martina |
Minovski, Nikola
Topics
Farmacevtska kemija |
bacterial type II topoisomerases |
DNA gyrase |
topoisomerase IV |
NBTIs |
hERG |
tertiary amine |
topoizomeraze bakterijskega tipa II |
DNA girazetopoizomeraza IV |
terciarni amin |
monoamin oksidaza B |
inhibitorji |
nevroblastom celična linija
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Author | Kokot, Maja, 1995- ... |
Title | Diminishing hERG inhibitory activity of aminopiperidine-naphthyridine linked NBTI antibacterials by structural and physicochemical optimizations |
Publication date | 2022-11-30 |
COBISS.SI-ID | 118137091 |
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 | P1-0208-2022 |
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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Kokot, Maja, 1995- | 53608 |
Weiss, Matjaž | 50503 |
Zdovc, Irena | 12682 |
Anderluh, Marko | 21456 |
Hrast, Martina | 32036 |
Minovski, Nikola | 29497 |
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