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New N-phenylpyrrolamide DNA gyrase B inhibitors : optimisation of efficacy and antibacterial activityDurcik, Martina ...The ATP binding site located on the subunit B of DNA gyrase is an attractive target for the development of new antibacterial agents. In recent decades, several small-molecule inhibitor classes have ... been discovered but none has so far reached the market. We present here the discovery of a promising new series of N-phenylpyrrolamides with low nanomolar IC50 values against DNA gyrase, and submicromolar IC50 values against topoisomerase IV from Escherichia coli and Staphylococcus aureus. The most potent compound in the series has an IC50 value of 13nM against E. coli gyrase. Minimum inhibitory concentrations (MICs) against Gram-positive bacteria are in the low micromolar range. The oxadiazolone derivative 11a, with an IC50 value of 85nM against E. coli DNA gyrase displays the most potent antibacterial activity, with MIC values of 1.56 microM against Enterococcus faecalis, and 3.13 microM against wild type S. aureus, methicillin-resistant S. aureus (MRSA) and vancomycin-resistant Enterococcus (VRE). The activity against wild type E. coli in the presence of efflux pump inhibitor phenylalanine-arginine beta-naphthylamide (PA(beta)N) is 4.6microM.Source: European journal of medicinal chemistry. - ISSN 0223-5234 (Vol. 154, June 2018, str. 117-132)Type of material - article, component part ; adult, seriousPublish date - 2018Language - englishCOBISS.SI-ID - 4504945
Link(s):
https://www.sciencedirect.com/science/article/pii/S022352341830415XDostop preko računalnikov UL
DOI
Author
Durcik, Martina |
Lovison, Denise |
Skok, Žiga, farmacevt |
Durante Cruz, Cristina |
Tammela, Päivi |
Tomašič, Tihomir |
Benedetto Tiz, Davide |
Draskovits, Gábor |
Nyerges, Ákos |
Pál, Csaba |
Ilaš, Janez |
Peterlin-Mašič, Lucija |
Kikelj, Danijel |
Zidar, Nace
Topics
Bakterijska rezistenca |
antibacterial |
DNA gyrase |
GyrB |
inhibitor |
N-phenylpyrrolamide |
ParE |
tTopoisomerase IV
Author | Durcik, Martina ... |
Title | New N-phenylpyrrolamide DNA gyrase B inhibitors : optimisation of efficacy and antibacterial activity |
Publication date | 2018-06-25 |
COBISS.SI-ID | 4504945 |
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 |
---|---|---|---|
Farmacevtska kemija: načrtovanje, sinteza in vrednotenje učinkovin | P1-0208-2015 |
Javna agencija za znanstvenoraziskovalno in inovacijsko dejavnost Republike Slovenije |
|
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 |
|
New antimicrobials against Gram-positive bacteria | 304697 |
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 | 312503 |
Academy of Finland |
|
Bacterial evolution of hypersensitivity and resistance against antimicrobial peptides | resistance evolution | 648364 |
European Commission |
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https://www.sciencedirect.com/science/article/pii/S022352341830415X |
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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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Durcik, Martina | 50490 |
Lovison, Denise | |
Skok, Žiga, farmacevt | 39202 |
Durante Cruz, Cristina | |
Tammela, Päivi | |
Tomašič, Tihomir | 28334 |
Benedetto Tiz, Davide | 57300 |
Draskovits, Gábor | |
Nyerges, Ákos | |
Pál, Csaba | |
Ilaš, Janez | 24400 |
Peterlin-Mašič, Lucija | 19317 |
Kikelj, Danijel | 01463 |
Zidar, Nace | 28905 |
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