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New N-phenyl-4,5-dibromopyrrolamides as DNA gyrase B inhibitorsZidar, Nace ...Due to the rapid development of antimicrobial resistance, the discovery of new antibacterials is essential in the fight against potentially lethal infections. The DNA gyrase B (GyrB) subunit of ... bacterial DNA gyrase is an excellent target for the design of antibacterials, as it has been clinically validated by novobiocin. However, there are currently no drugs in clinical use that target GyrB. We prepared a new series of N-phenyl-4,5-dibromopyrrolamides and evaluated them against DNA gyrase and against the structurally and functionally similar enzyme, topoisomerase IV. The most active compound, 28, had an IC50 of 20 nM against Escherichia coli DNA gyrase. The IC50 values of 28 against Staphylococcus aureus DNA gyrase, and E. coli and S. aureus topoisomerase IV were in the low micromolar range. However, the compounds evaluated did not show significant antibacterial activities against selected Gram-positive and Gram-negative bacteria. Our results indicate that for potent inhibition of DNA gyrase, a combination of polar groups on the carboxylic end of the molecule and substituents that reach into the ''lipophilic floor'' of the enzyme is required.Source: MedChemComm. - ISSN 2040-2503 (Vol. 10, iss. 6, 2019, str. 1007-1017)Type of material - article, component partPublish date - 2019Language - englishCOBISS.SI-ID - 4724337
Author | Zidar, Nace ... |
Title | New N-phenyl-4,5-dibromopyrrolamides as DNA gyrase B inhibitors |
Publication date | 2019-06-01 |
COBISS.SI-ID | 4724337 |
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 |
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Phenotypic biosensor-based HTS and mode of action analysis by metabolomics and transcriptomics for enhancing antimicrobial drug discovery against Gram-negative bacteria | 312503 |
Academy of Finland |
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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 |
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New antimicrobials against Gram-positive bacteria | 304697 |
Academy of Finland |
Files that belong to the publication
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https://pubs.rsc.org/en/content/articlelanding/2019/md/c9md00224c#!divAbstract |
https://pubs.rsc.org/en/content/articlepdf/2019/md/c9md00224c?page=search |
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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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Zidar, Nace | 28905 |
Macut, Helena | 37477 |
Tomašič, Tihomir | 28334 |
Peterlin-Mašič, Lucija | 19317 |
Ilaš, Janez | 24400 |
Zega, Anamarija | 18633 |
Tammela, Päivi | |
Kikelj, Danijel | 01463 |
Source: Personal bibliographies
and: SICRIS
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