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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.Vir: European journal of medicinal chemistry. - ISSN 0223-5234 (Vol. 154, June 2018, str. 117-132)Vrsta gradiva - članek, sestavni del ; neleposlovje za odrasleLeto - 2018Jezik - angleškiCOBISS.SI-ID - 4504945
Povezava(-e):
https://www.sciencedirect.com/science/article/pii/S022352341830415XDostop preko računalnikov UL
DOI
Avtor
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
Teme
Bakterijska rezistenca |
antibacterial |
DNA gyrase |
GyrB |
inhibitor |
N-phenylpyrrolamide |
ParE |
tTopoisomerase IV
Avtor | Durcik, Martina ... |
Naslov | New N-phenylpyrrolamide DNA gyrase B inhibitors : optimisation of efficacy and antibacterial activity |
Datum objave | 2018-06-25 |
COBISS.SI-ID | 4504945 |
Verzija objave v repozitoriju | Založnikova različica |
Licenca objave v repozitoriju | Ni določeno |
Embargo | Takojšnja javna objava |
Projekti, iz katerih je bila financirana objava
Naziv | Akronim | Številka projekta | Financer |
---|---|---|---|
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 |
Datoteke, ki spadajo k objavi
Povezava |
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https://www.sciencedirect.com/science/article/pii/S022352341830415X |
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JCR | SNIP | JCR | SNIP | JCR | SNIP | JCR | SNIP |
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Ime baze podatkov | Področje | Leto |
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Povezave do osebnih bibliografij avtorjev | Povezave do podatkov o raziskovalcih v sistemu SICRIS |
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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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