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Improved N-phenylpyrrolamide inhibitors of DNA gyrase as antibacterial agents for high-priority bacterial strains [Elektronski vir]Zidar, Nace ...In this work, we describe an improved series of N-phenylpyrrolamide inhibitors that exhibit potent activity against DNA gyrase and are highly effective against high-priority gram-positive bacteria. ... The most potent compounds show low nanomolar IC50 values against Escherichia coli DNA gyrase, and in addition, compound 7c also inhibits E. coli topoisomerase IV in the nanomolar concentration range, making it a promising candidate for the development of potent dual inhibitors for these enzymes. All tested compounds show high selectivity towards the human isoform DNA topoisomerase IIα. Compounds 6a, 6d, 6e and 6f show MIC values between 0.031 and 0.0625 μg/mL against vancomycin-intermediate S. aureus (VISA) and Enterococcus faecalis strains. Compound 6g shows an inhibitory effect against the methicillin-resistant S. aureus strain (MRSA) with a MIC of 0.0625 μg/mL and against the E. faecalis strain with a MIC of 0.125 μg/mL. In a time-kill assay, compound 6d showed a dose-dependent bactericidal effect on the MRSA strain and achieved bactericidal activity at 8 × MIC after 8 h. The duration of the post-antibiotic effect (PAE) on the MRSA strain for compound 6d was 2 h, which corresponds to the PAE duration for ciprofloxacin. The compounds were not cytotoxic at effective concentrations, as determined in an MTS assay on the MCF-7 breast cancer cell line.Source: European journal of medicinal chemistry [Elektronski vir]. - ISSN 1768-3254 (Vol. 278, 2024, 19 str.)Type of material - e-article ; adult, seriousPublish date - 2024Language - englishCOBISS.SI-ID - 206357251
Author
Zidar, Nace |
Onali, Alessia |
Peršolja, Peter |
Benedetto Tiz, Davide |
Dernovšek, Jaka |
Skok, Žiga, farmacevt |
Durcik, Martina |
Cotman, Andrej Emanuel |
Hrast, Martina |
Zega, Anamarija |
Peterlin-Mašič, Lucija |
Ilaš, Janez |
Tomašič, Tihomir |
Kikelj, Danijel
Topics
Farmacevtska kemija |
antibacterial |
DNA gyrase |
GyrB |
inhibitor |
N-phenylpyrrolamide |
ParE |
topoisomerase IV |
antibakterijski zaviralci |
DNA giraze |
GyrB |
N-fenilpirolamid |
ParE |
topoizomeraza IV
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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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Zidar, Nace | 28905 |
Onali, Alessia | ![]() |
Peršolja, Peter | 26104 |
Benedetto Tiz, Davide | 57300 |
Dernovšek, Jaka | 54784 |
Skok, Žiga, farmacevt | 39202 |
Durcik, Martina | 50490 |
Cotman, Andrej Emanuel | 37459 |
Hrast, Martina | 32036 |
Zega, Anamarija | 18633 |
Peterlin-Mašič, Lucija | 19317 |
Ilaš, Janez | 24400 |
Tomašič, Tihomir | 28334 |
Kikelj, Danijel | 01463 |
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