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An optimised series of substituted N-phenylpyrrolamides as DNA gyrase B inhibitorsBenedetto Tiz, Davide ...ATP competitive inhibitors of DNA gyrase and topoisomerase IV have great therapeutic potential, but none of the described synthetic compounds has so far reached the market. To optimise the activities ... and physicochemical properties of our previously reported N-phenylpyrrolamide inhibitors, we have synthesized an improved, chemically variegated selection of compounds and evaluated them against DNA gyrase and topoisomerase IV enzymes, and against selected Gram-positive and Gram-negative bacteria. The most potent compound displayed IC50 values of 6.9%nM against Escherichia coli DNA gyrase and 960%nM against Staphylococcus aureus topoisomerase IV. Several compounds displayed minimum inhibitory concentrations (MICs) against Gram-positive strains in the 1-50%%M range, one of which inhibited the growth of Enterococcus faecalis, Enterococcus faecium, S. aureus and Streptococcus pyogenes with MIC values of 1.56%%M, 1.56%%M, 0.78%%M and 0.72%%M, respectively. This compound has been investigated further on methicillin-resistant S. aureus (MRSA) and on ciprofloxacin non-susceptible and extremely drug resistant strain of S. aureus (MRSA VISA). It exhibited the MIC value of 2.5%%M on both strains, and MIC value of 32%%M against MRSA in the presence of inactivated human blood serum. Further studies are needed to confirm its mode of action.Source: European journal of medicinal chemistry. - ISSN 0223-5234 (Vol. 167, Apr. 2019, str. 269-290)Type of material - article, component part ; adult, seriousPublish date - 2019Language - englishCOBISS.SI-ID - 4686961
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https://www.sciencedirect.com/science/article/pii/S022352341930114X?via%3Dihub#!Dostop preko računalnikov UL
DOI
Author
Benedetto Tiz, Davide |
Skok, Žiga, farmacevt |
Durcik, Martina |
Tomašič, Tihomir |
Peterlin-Mašič, Lucija |
Ilaš, Janez |
Zega, Anamarija |
Draskovits, Gábor |
Revesz, T. |
Nyerges József, Ákos |
Pál, Csaba |
Durante Cruz, Cristina |
Tammela, Päivi |
Žigon, Dušan |
Kikelj, Danijel |
Zidar, Nace
Topics
Bakterijska rezistenca |
antibacterial |
DNA gyrase |
GyrB |
inhibitor |
ATP competitive |
N-phenylpyrrolamide |
tTopoisomerase IV |
parE
Author | Benedetto Tiz, Davide ... |
Title | An optimised series of substituted N-phenylpyrrolamides as DNA gyrase B inhibitors |
Publication date | 2019-04-01 |
COBISS.SI-ID | 4686961 |
Publication version in repository | Publisher's version |
Publication licence | Creative Commons Attribution 4.0 International |
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 |
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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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Benedetto Tiz, Davide | 57300 |
Skok, Žiga, farmacevt | 39202 |
Durcik, Martina | 50490 |
Tomašič, Tihomir | 28334 |
Peterlin-Mašič, Lucija | 19317 |
Ilaš, Janez | 24400 |
Zega, Anamarija | 18633 |
Draskovits, Gábor | |
Revesz, T. | |
Nyerges József, Ákos | |
Pál, Csaba | |
Durante Cruz, Cristina | |
Tammela, Päivi | |
Žigon, Dušan | 03950 |
Kikelj, Danijel | 01463 |
Zidar, Nace | 28905 |
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