[HTML][HTML] DNA topoisomerase inhibitors: trapping a DNA-cleaving machine in motion

BD Bax, G Murshudov, A Maxwell, T Germe - Journal of molecular biology, 2019 - Elsevier
Type II topoisomerases regulate DNA topology by making a double-stranded break in one
DNA duplex, transporting another DNA segment through this break and then resealing it …

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 …

Synthesis of monofluoroalkenes: a leap forward

M Drouin, JD Hamel, JF Paquin - Synthesis, 2018 - thieme-connect.com
Monofluoroalkenes have found wide application in organic chemistry, medicinal chemistry,
and materials science. This review summarizes the most recent advances made regarding …

BWC0977, a broad-spectrum antibacterial clinical candidate to treat multidrug resistant infections

S Hameed P, H Kotakonda, S Sharma… - Nature …, 2024 - nature.com
The global crisis of antimicrobial resistance (AMR) necessitates the development of broad-
spectrum antibacterial drugs effective against multi-drug resistant (MDR) pathogens …

Two Decades of Successful SAR-Grounded Stories of the Novel Bacterial Topoisomerase Inhibitors (NBTIs) Miniperspective

A Kolarič, M Anderluh, N Minovski - Journal of medicinal …, 2020 - ACS Publications
The emergence of bacterial resistance against life-saving medicines has forced the scientific
community and pharmaceutical industry to take actions in the quest for novel antibacterials …

A 2.8 Å Structure of Zoliflodacin in a DNA Cleavage Complex with Staphylococcus aureus DNA Gyrase

H Morgan, M Lipka-Lloyd, AJ Warren… - International Journal of …, 2023 - mdpi.com
Since 2000, some thirteen quinolones and fluoroquinolones have been developed and
have come to market. The quinolones, one of the most successful classes of antibacterial …

Design, Synthesis, in vitro and in silico Characterization of 2‐Quinolone‐L‐alaninate‐1,2,3‐triazoles as Antimicrobial Agents

O Moussaoui, R Bhadane, R Sghyar, J Ilaš… - …, 2022 - Wiley Online Library
Due to the ever‐increasing antimicrobial resistance there is an urgent need to continuously
design and develop novel antimicrobial agents. Inspired by the broad antibacterial activities …

[HTML][HTML] Novel bacterial topoisomerase inhibitors (NBTIs)–a comprehensive review

J Desai, S Sachchidanand, S Kumar… - European Journal of …, 2021 - Elsevier
Bacterial DNA gyrase and topoisomerase IV inhibition has emerged as a promising strategy
for the cure of infections caused by antibiotic-resistant bacteria. Small molecule …

Synergistic Effect of Hydralazine Associated with Triazoles on Candida spp. in Planktonic Cells

FBSA do Nascimento, LGA Valente Sá… - Future …, 2023 - Taylor & Francis
Objective: To evaluate the antifungal activity of hydralazine hydrochloride alone and in
synergy with azoles against Candida spp. and the action mechanism. Methods: We used …

Novel tricyclics (eg, GSK945237) as potent inhibitors of bacterial type IIA topoisomerases

TJ Miles, AJ Hennessy, B Bax, G Brooks… - Bioorganic & medicinal …, 2016 - Elsevier
During the course of our research on the lead optimisation of the NBTI (Novel Bacterial Type
II Topoisomerase Inhibitors) class of antibacterials, we discovered a series of tricyclic …