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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.Source: Bioorganic chemistry. - ISSN 0045-2068 (Vol. 95, 2020, str. 1-13)Type of material - article, component part ; adult, seriousPublish date - 2020Language - englishCOBISS.SI-ID - 4865137
Author
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
Topics
Bakterijska rezistenca |
Antibiotiki |
antibiotics |
Catechol |
DNA gyrase |
Siderophore mimic |
inhibitors
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Author | Lamut, Andraž ... |
Title | Design, synthesis and biological evaluation of novel DNA gyrase inhibitorsand their siderophore mimic conjugates |
Publication date | 2020-01-11 |
COBISS.SI-ID | 4865137 |
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 |
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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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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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