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Št. zadetkov: 3
Rational design of balanced dual-targeting antibiotics with limited resistance
Ákos Nyerges, Tihomir Tomašić, Martina Durcik, Tamás Révész, Petra Éva Szili, Žiga Skok, Nace Zidar, Janez Ilaš, Anamarija Zega, Danijel Kikelj, Lucija Peterlin-Mašič
Izvirni znanstveni članek
Oznake: antibiotics;bacterial resistance;bacterial targets;
Antibiotics that inhibit multiple bacterial targets offer a promising therapeutic strategy against resistance evolution, but developing such antibiotics is challenging. Here we demonstrate that a rational design of balanced multitargeting antibiotics is feasible by using a medicinal chemistry workfl ...
Leto: 2020 Vir: Fakulteta za farmacijo (UL FFA)
Exploring the 5-substituted 2-aminobenzothiazole-based DNA gyrase B inhibitors active against ESKAPE pathogens
Maša Sterle, Martina Durcik, Clare E. M. Stevenson, Sara R. Henderson, Petra Eva Szili, Marton Czikkely, David M. Lawson, Danijel Kikelj, Nace Zidar, Lucija Peterlin-Mašič, Janez Ilaš, Tihomir Tomašić, Andrej Emanuel Cotman, Anamarija Zega
Izvirni znanstveni članek
Oznake: inhibitorji;organske kisline;proteini;bacteria;genetics;inhibitors;organic acids;peptides;proteins;
We present a new series of 2-aminobenzothiazole-based DNA gyrase B inhibitors with promising activity against ESKAPE bacterial pathogens. Based on the binding information extracted from the cocrystal structure of DNA gyrase B inhibitor A, in complex with Escherichia coli GyrB24, we expanded the chem ...
Leto: 2023 Vir: Fakulteta za farmacijo (UL FFA)
Hybrid inhibitors of DNA gyrase A and B
Martina Durcik, Žiga Skok, Janez Ilaš, Nace Zidar, Anamarija Zega, Petra Éva Szili, Gábor Draskovits, Tamás Révész, Danijel Kikelj, Ákos Nyerges, Csaba Pál, Lucija Peterlin-Mašič, Tihomir Tomašić
Izvirni znanstveni članek
Oznake: antibacterial;ciprofloxacin;DNA gyrase;dual inhibitor;hybrid;
The discovery of multi-targeting ligands of bacterial enzymes is an important strategy to combat rapidly spreading antimicrobial resistance. Bacterial DNA gyrase and topoisomerase IV are validated targets for the development of antibiotics. They can be inhibited at their catalytic sites or at their ...
Leto: 2021 Vir: Fakulteta za farmacijo (UL FFA)
Št. zadetkov: 3
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