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Synthesis and evaluation of N-phenylpyrrolamides as DNA gyrase B inhibitors [Elektronski vir]Durcik, Martina ...ATP-competitive inhibitors of DNA gyrase and topoisomerase IV are among the most interesting classes of antibacterial drugs that are unrepresented in the antibacterial pipeline. We developed 32 new ... N-phenylpyrrolamides and evaluated them against DNA gyrase and topoisomerase IV from E. coli and Staphylococcus aureus. Antibacterial activities were studied against Gram-positive and Gram-negative bacterial strains. The most potent compound displayed an IC50 of 47micro nm against E.coli DNA gyrase, and a minimum inhibitory concentration (MIC) of 12.5 microm against the Gram-positive Enterococcus faecalis. Some compounds displayed good antibacterial activities against an efflux-pump-deficient E. coli strain (MIC=6.25 microm) and against wild-type E. coli in the presence of efflux pump inhibitor PAbetaN (MIC=3.13 microm). Here we describe new findings regarding the structure-activity relationships of N-phenylpyrrolamide DNA gyrase B inhibitors and investigate the factors that are important for the antibacterial activity of this class of compounds.Source: ChemMedChem. - ISSN 1860-7187 (Vol. 13, iss. 2, 2018, str. 186-198)Type of material - e-articlePublish date - 2018Language - englishCOBISS.SI-ID - 4461681
Author
Durcik, Martina |
Tammela, Päivi |
Barančokova, Michaela |
Tomašič, Tihomir |
Ilaš, Janez |
Kikelj, Danijel |
Zidar, Nace
Topics
DNA gyrase |
GyrB |
antibacterials |
inhibitors |
pyrrolamides
Author | Durcik, Martina ... |
Title | Synthesis and evaluation of N-phenylpyrrolamides as DNA gyrase B inhibitors [Elektronski vir] |
Publication date | 2018-01-22 |
COBISS.SI-ID | 4461681 |
Publication version in repository | Publisher's version |
Publication licence | Unidentified |
Embargo | Immediate publication for public |
Project(s) from which the publication was funded
Title | Acronym | Project ID | Funder |
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Farmacevtska kemija: načrtovanje, sinteza in vrednotenje učinkovin | P1-0208-2015 |
Javna agencija za znanstvenoraziskovalno in inovacijsko dejavnost Republike Slovenije |
|
Interdisciplinary Training Network for Validation of Gram-Negative Antibacterial Targets | INTEGRATE | 642620 |
European Commission |
Phenotypic biosensor-based HTS and mode of action analysis by metabolomics and transcriptomics for enhancing antimicrobial drug discovery against Gram-negative bacteria | 277001 |
Academy of Finland |
|
Phenotypic biosensor-based HTS and mode of action analysis by metabolomics and transcriptomics for enhancing antimicrobial drug discovery against Gram-negative bacteria | 284477 |
Academy of Finland |
Files that belong to the publication
Link |
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https://onlinelibrary.wiley.com/doi/10.1002/cmdc.201700549 |
https://onlinelibrary.wiley.com/doi/epdf/10.1002/cmdc.201700549 |
https://repozitorij.uni-lj.si/IzpisGradiva.php?id=106642 |
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DRS, in which the journal is indexed
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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Durcik, Martina | 50490 |
Tammela, Päivi | |
Barančokova, Michaela | 39784 |
Tomašič, Tihomir | 28334 |
Ilaš, Janez | 24400 |
Kikelj, Danijel | 01463 |
Zidar, Nace | 28905 |
Source: Personal bibliographies
and: SICRIS
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