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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.Vir: European journal of medicinal chemistry. - ISSN 0223-5234 (Vol. 167, Apr. 2019, str. 269-290)Vrsta gradiva - članek, sestavni del ; neleposlovje za odrasleLeto - 2019Jezik - angleškiCOBISS.SI-ID - 4686961
Povezava(-e):
https://www.sciencedirect.com/science/article/pii/S022352341930114X?via%3Dihub#!Dostop preko računalnikov UL
DOI
Avtor
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
Teme
Bakterijska rezistenca |
antibacterial |
DNA gyrase |
GyrB |
inhibitor |
ATP competitive |
N-phenylpyrrolamide |
tTopoisomerase IV |
parE
Avtor | Benedetto Tiz, Davide ... |
Naslov | An optimised series of substituted N-phenylpyrrolamides as DNA gyrase B inhibitors |
Datum objave | 2019-04-01 |
COBISS.SI-ID | 4686961 |
Verzija objave v repozitoriju | Založnikova različica |
Licenca objave v repozitoriju | Creative Commons Priznanje avtorstva 4.0 Mednarodna |
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 |
Datoteke, ki spadajo k objavi
Povezava |
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https://www.sciencedirect.com/science/article/pii/S022352341930114X?via%3Dihub#! |
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JCR | SNIP | JCR | SNIP | JCR | SNIP | JCR | SNIP |
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Povezave do osebnih bibliografij avtorjev | Povezave do podatkov o raziskovalcih v sistemu SICRIS |
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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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