Thiazoles, their benzofused systems, and thiazolidinone derivatives: versatile and promising tools to combat antibiotic resistance

S Cascioferro, B Parrino, D Carbone… - Journal of medicinal …, 2020 - ACS Publications
Thiazoles, their benzofused systems, and thiazolidinone derivatives are widely recognized
as nuclei of great value for obtaining molecules with various biological activities, including …

ATP-competitive DNA gyrase and topoisomerase IV inhibitors as antibacterial agents

M Durcik, T Tomašič, N Zidar, A Zega… - Expert opinion on …, 2019 - Taylor & Francis
Introduction: The bacterial topoisomerases DNA gyrase and topoisomerase IV are validated
targets for development of novel antibacterial agents. Fluoroquinolones inhibit the catalytic …

Antibiofilm, antimicrobial, anti-quorum sensing, and antioxidant activities of Saudi Sidr Honey: in vitro and molecular docking studies

AS Bazaid, A Alsolami, M Patel, AM Khateb… - Pharmaceutics, 2023 - mdpi.com
Sidr honey is a valuable source of bioactive compounds with promising biological
properties. In the present study, antimicrobial, antioxidant, and anti-quorum sensing …

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 …

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 …

Identification of Potent DNA Gyrase Inhibitors Active against Mycobacterium tuberculosis

B Pakamwong, P Thongdee, B Kamsri… - Journal of Chemical …, 2022 - ACS Publications
Mycobacterium tuberculosis DNA gyrase manipulates the DNA topology using controlled
breakage and religation of DNA driven by ATP hydrolysis. DNA gyrase has been validated …

Identification of promising anti-DNA gyrase antibacterial compounds using de novo design, molecular docking and molecular dynamics studies

MA Islam, TS Pillay - Journal of Biomolecular Structure and …, 2020 - Taylor & Francis
The rapidly increasing rate of antibiotic resistance is of great concern. Approximately two
million deaths result annually from bacterial infections worldwide. Therefore, there is a …

Advancement of GyrB Inhibitors for Treatment of Infections Caused by Mycobacterium tuberculosis and Non-tuberculous Mycobacteria

SS Stokes, R Vemula, MJ Pucci - ACS Infectious Diseases, 2020 - ACS Publications
The prospect of ever increasing antibiotic resistance eroding currently available treatment
options for bacterial infections underscores the need to continue to identify new antibiotics …

An optimised series of substituted N-phenylpyrrolamides as DNA gyrase B inhibitors

DB Tiz, Ž Skok, M Durcik, T Tomašič, LP Mašič… - European journal of …, 2019 - Elsevier
ATP competitive inhibitors of DNA gyrase and topoisomerase IV have great therapeutic
potential, but none of the described synthetic compounds has so far reached the market. To …

Total synthesis of kibdelomycin

C He, Y Wang, C Bi, DS Peters… - Angewandte …, 2022 - Wiley Online Library
A modular total synthesis of kibdelomycin is disclosed that should enable structure–activity
relationship (SAR) studies of this interesting class of antibiotics. The route uses simple …