Literature

Abstract

There is an urgent and unmet medical need for new antibacterial drugs that tackle infections caused by multidrug-resistant (MDR) pathogens. During the course of our wider efforts to discover and exploit novel mechanism of action antibacterials, we have identified a novel series of isothiazolone based inhibitors of bacterial type II topoisomerase. Compounds from the class displayed excellent activity against both Gram-positive and Gram-negative bacteria with encouraging activity against a panel of MDR clinical Escherichia coli isolates when compared to ciprofloxacin. Representative compounds also displayed a promising in vitro safety profile.

DOI： 10.1016/j.bmcl.2016.07.061

Discovery and structure–activity relationships of a novel isothiazolone class of bacterial type II topoisomerase inhibitors

Bioorganic & Medicinal Chemistry Letters 2016.0

Discovery and structure–activity relationships of a novel oxazolidinone class of bacterial type II topoisomerase inhibitors

Bioorganic & Medicinal Chemistry Letters 2022.0

Tetrahydroindazole inhibitors of bacterial type II topoisomerases. Part 2: SAR development and potency against multidrug-resistant strains

Bioorganic & Medicinal Chemistry Letters 2007.0

Discovery and Optimization of Indolyl-Containing 4-Hydroxy-2-Pyridone Type II DNA Topoisomerase Inhibitors Active against Multidrug Resistant Gram-negative Bacteria

Journal of Medicinal Chemistry 2018.0

Novel coumarin-pyrazole carboxamide derivatives as potential topoisomerase II inhibitors: Design, synthesis and antibacterial activity

European Journal of Medicinal Chemistry 2018.0

Novel quinoline derivatives as inhibitors of bacterial DNA gyrase and topoisomerase IV