Recent advances in DNA gyrase-targeted antimicrobial agents

SN Dighe, TA Collet - European Journal of Medicinal Chemistry, 2020 - Elsevier
Antimicrobial resistance is one of the greatest challenges facing the world today. In the
United States alone, it is responsible for the death of more than 20,000 people each year …

Recent progress in the discovery and development of DNA gyrase B inhibitors

M Barančoková, D Kikelj, J Ilaš - Future medicinal chemistry, 2018 - Taylor & Francis
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 …

Discovery of benzothiazole scaffold-based DNA gyrase B inhibitors

M Gjorgjieva, T Tomasic, M Barancokova… - Journal of medicinal …, 2016 - ACS Publications
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 …

3D-QSAR and docking studies of flavonoids as potent Escherichia coli inhibitors

Y Fang, Y Lu, X Zang, T Wu, XJ Qi, S Pan, X Xu - Scientific Reports, 2016 - nature.com
Flavonoids are potential antibacterial agents. However, key substituents and mechanism for
their antibacterial activity have not been fully investigated. The quantitative structure-activity …

New dual inhibitors of bacterial topoisomerases with broad-spectrum antibacterial activity and in vivo efficacy against vancomycin-intermediate Staphylococcus …

M Durcik, AE Cotman, Z Toplak, S Mozina… - Journal of medicinal …, 2023 - ACS Publications
A new series of dual low nanomolar benzothiazole inhibitors of bacterial DNA gyrase and
topoisomerase IV were developed. The resulting compounds show excellent broad …

Discovery and hit-to-lead optimization of benzothiazole scaffold-based DNA gyrase inhibitors with potent activity against Acinetobacter baumannii and Pseudomonas …

AE Cotman, M Durcik, D Benedetto Tiz… - Journal of medicinal …, 2023 - ACS Publications
We have developed compounds with a promising activity against Acinetobacter baumannii
and Pseudomonas aeruginosa, which are both on the WHO priority list of antibiotic-resistant …

Discovery of substituted oxadiazoles as a novel scaffold for DNA gyrase inhibitors

Ž Jakopin, J Ilaš, M Barančoková, M Brvar… - European Journal of …, 2017 - Elsevier
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 …

Ir-Catalyzed Asymmetric Cascade Allylation/Spiroketalization Reaction for Stereoselective Synthesis of Oxazoline-Spiroketals

H Yan, X Shao, X Xu, Z Li, WL Yang - Organic Letters, 2023 - ACS Publications
An asymmetric cascade allylation/spiroketalization reaction between 2-(1-hydroxyallyl)
phenols and 5-methyleneoxazolines is accomplished by using a chiral Ir (I) catalyst derived …

Exploring the chemical space of benzothiazole-based DNA gyrase B inhibitors

Z Skok, M Barančoková, O Benek… - ACS medicinal …, 2020 - ACS Publications
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 …

Synthesis and Evaluation of N‐Phenylpyrrolamides as DNA Gyrase B Inhibitors

M Durcik, P Tammela, M Barančoková… - …, 2018 - Wiley Online Library
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 …