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Design, synthesis and biological evaluation of novel DNA gyrase inhibitorsand their siderophore mimic conjugatesLamut, Andraž ...Bacterial DNA gyrase is an important target for the development of novel antibacterial drugs, which are urgently needed because of high level of antibiotic resistance worldwide. We designed and ... synthesized new 4,5,6,7-tetrahydrobenzo[d]thiazole-based DNA gyrase B inhibitors and their conjugates with siderophore mimics, which were introduced to increase the uptake of inhibitors into the bacterial cytoplasm. The most potent conjugate 34 had an IC50 of 58 nM against Escherichia coli DNA gyrase and displayed MIC of 14 [micro]g/mL against E. coli [micro]tolC strain. Only minor improvements in the antibacterial activities against wild-type E. coli in low-iron conditions were seen for DNA gyrase inhibitor - siderophore mimic conjugates.Vir: Bioorganic chemistry. - ISSN 0045-2068 (Vol. 95, 2020, str. 1-13)Vrsta gradiva - članek, sestavni del ; neleposlovje za odrasleLeto - 2020Jezik - angleškiCOBISS.SI-ID - 4865137
Avtor
Lamut, Andraž |
Durante Cruz, Cristina |
Skok, Žiga, farmacevt |
Barančokova, Michaela |
Zidar, Nace |
Zega, Anamarija |
Peterlin-Mašič, Lucija |
Ilaš, Janez |
Tammela, Päivi |
Kikelj, Danijel |
Tomašič, Tihomir
Teme
Bakterijska rezistenca |
Antibiotiki |
antibiotics |
Catechol |
DNA gyrase |
Siderophore mimic |
inhibitors
Avtor | Lamut, Andraž ... |
Naslov | Design, synthesis and biological evaluation of novel DNA gyrase inhibitorsand their siderophore mimic conjugates |
Datum objave | 2020-01-11 |
COBISS.SI-ID | 4865137 |
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 |
Datoteke, ki spadajo k objavi
Povezava |
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https://www.sciencedirect.com/science/article/pii/S0045206819316591?dgcid=author |
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JCR | SNIP | JCR | SNIP | JCR | SNIP | JCR | SNIP |
Baze podatkov, v katerih je revija indeksirana
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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Lamut, Andraž | 37669 |
Durante Cruz, Cristina | |
Skok, Žiga, farmacevt | 39202 |
Barančokova, Michaela | 39784 |
Zidar, Nace | 28905 |
Zega, Anamarija | 18633 |
Peterlin-Mašič, Lucija | 19317 |
Ilaš, Janez | 24400 |
Tammela, Päivi | |
Kikelj, Danijel | 01463 |
Tomašič, Tihomir | 28334 |
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