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Št. zadetkov: 6
Recent progress in the discovery and development of DNA gyrase B inhibitors
Michaela Barančokova, Danijel Kikelj, Janez Ilaš
Pregledni znanstveni članek
Oznake: zaviralci giraze B;topoizomeraza IV;akademske raziskave;
New antibacterials that modulate less explored targets are needed to fight the emerging bacterial resistance. DNA gyrase and topoisomerase IV are attractive targets in this search. These are both type II topoisomerases that can cleave both DNA strands, and can thus alter DNA topology during replicat ...
Leto: 2018 Vir: Fakulteta za farmacijo (UL FFA)
Design, synthesis and biological evaluation of 4,5-dibromo-N-(thiazol-2-yl)-1H-pyrrole-2-carboxamide derivatives as novel DNA gyrase inhibitors
Tihomir Tomašić, Matic Mirt, Michaela Barančokova, Janez Ilaš, Nace Zidar, Päivi Tammela, Danijel Kikelj
Izvirni znanstveni članek
Oznake: antibacterial;DNA gyrase;docking;inhibitor;thiazole;
Development of novel DNA gyrase B inhibitors is an important field of antibacterial drug discovery whose aim is to introduce a more effective representative of this mechanistic class into the clinic. In the present study, two new series of Escherichia coli DNA gyrase inhibitors bearing the 4,5-dibro ...
Leto: 2017 Vir: Fakulteta za farmacijo (UL FFA)
Synthesis and evaluation of N-phenylpyrrolamides as DNA gyrase B inhibitors
Martina Durcik, Päivi Tammela, Michaela Barančokova, Tihomir Tomašić, Janez Ilaš, Danijel Kikelj, Nace Zidar
Izvirni znanstveni članek
Oznake: DNA gyrase;GyrB;antibacterials;inhibitors;pyrrolamides;
ATP-competitive inhibitors of DNA gyrase and topoisomerase IV are among the most interesting classes of antibacterial drugs that are unrepresented in the antibacterial pipeline. We developed 32 new N-phenylpyrrolamides and evaluated them against DNA gyrase and topoisomerase IV from E. coli and Staph ...
Leto: 2018 Vir: Fakulteta za farmacijo (UL FFA)
Discovery of substituted oxadiazoles as a novel scaffold for DNA gyrase inhibitors
Žiga Jakopin, Janez Ilaš, Michaela Barančokova, Matjaž Brvar, Päivi Tammela, Marija Sollner Dolenc, Tihomir Tomašić, Danijel Kikelj
Izvirni znanstveni članek
Oznake: 1,2,4-oxadiazoles;DNA gyrase inhibition;topoisomerase IV inhibition;antibacterial screening;computer-aided drug design;
DNA gyrase and topoisomerase IV are type IIa topoisomerases that are essential bacterial enzymes required to oversee the topological state of DNA during transcription and replication processes. Their ATPase domains, GyrB and ParE, respectively, are recognized as viable targets for small molecule inh ...
Leto: 2017 Vir: Fakulteta za farmacijo (UL FFA)
Discovery of benzothiazole scaffold-based DNA gyrase B inhibitors
Marina Gjorgjieva, Tihomir Tomašić, Michaela Barančokova, Sotirios Katsamakas, Janez Ilaš, Päivi Tammela, Lucija Peterlin-Mašič, Danijel Kikelj
Izvirni znanstveni članek
Oznake: bioanorganska kemija;koordinacijske spojine;organorutenijevi kompleksi;diketonati;citotoksičnost;protirakava zdravila;organoruthenium complexes;diketonates;anticancer drugs;ROS;cytotoxicity;cell cycle arrest;
Bacterial DNA gyrase and topoisomerase IV control the topological state of DNA during replication and are validated targets for antibacterial drug discovery. Starting from our recently reported 4,5,6,7-tetrahydrobenzo[1,2-d]thiazole-based DNA gyrase B inhibitors, we replaced their central core with ...
Leto: 2016 Vir: Fakulteta za farmacijo (UL FFA)
Exploring the chemical space of benzothiazole-based DNA gyrase B inhibitors
Žiga Skok, Michaela Barančokova, Ondřej Benek, Cristina Durante Cruz, Päivi Tammela, Tihomir Tomašić, Nace Zidar, Lucija Peterlin-Mašič, Anamarija Zega, Danijel Kikelj, Janez Ilaš
Izvirni znanstveni članek
Oznake: DNA gyrase;topoisomerase IV;GyrB;ParE;antibacterial benzothiazole;
We designed and synthesized a series of inhibitors of the bacterial enzymes DNA gyrase and DNA topoisomerase IV, based on our recently published benzothiazole-based inhibitor bearing an oxalyl moiety. To improve the antibacterial activity and retain potent enzymatic activity, we systematically explo ...
Leto: 2020 Vir: Fakulteta za farmacijo (UL FFA)
Št. zadetkov: 6
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