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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.Vir: Bioorganic chemistry. - ISSN 0045-2068 (Vol. 128, 2022, 14 str.)Vrsta gradiva - članek, sestavni del ; neleposlovje za odrasleLeto - 2022Jezik - angleškiCOBISS.SI-ID - 118137091
Avtor
Kokot, Maja, 1995- |
Weiss, Matjaž |
Zdovc, Irena |
Anderluh, Marko |
Hrast, Martina |
Minovski, Nikola
Teme
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
Avtor | Kokot, Maja, 1995- ... |
Naslov | Diminishing hERG inhibitory activity of aminopiperidine-naphthyridine linked NBTI antibacterials by structural and physicochemical optimizations |
Datum objave | 2022-11-30 |
COBISS.SI-ID | 118137091 |
Verzija objave v repozitoriju | Založnikova različica |
Licenca objave v repozitoriju | Creative Commons Priznanje avtorstva 4.0 Mednarodna |
Embargo | Takojšnja javna objava |
Projekti, iz katerih je bila financirana objava
Naziv | Akronim | Številka projekta | Financer |
---|---|---|---|
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 |
Datoteke, ki spadajo k objavi
Povezava |
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https://www.sciencedirect.com/science/article/pii/S004520682200493X |
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Leto | Faktor vpliva | Izdaja | Kategorija | Razvrstitev | ||||
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JCR | SNIP | JCR | SNIP | JCR | SNIP | JCR | SNIP |
Baze podatkov, v katerih je revija indeksirana
Ime baze podatkov | Področje | Leto |
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Povezave do osebnih bibliografij avtorjev | Povezave do podatkov o raziskovalcih v sistemu SICRIS |
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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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