Article
Discovery and structure-activity relationships of a novel isothiazolone class of bacterial type II topoisomerase inhibitors.
Bioorganic & medicinal chemistry letters - 1 Sept 2016
Cooper Ian R, McCarroll Andrew J, McGarry David, Kirkham James, Pichowicz Mark, Walker Rolf, Warrilow Catherine, Salisbury Anne-Marie, Savage Victoria J, Moyo Emmanuel, Forward Henry, Cheung Jonathan, Metzger Richard, Gault Zoe, Nelson Gary, Hughes Diarmaid, Cao Sha, Maclean John, Charrier Cédric, Craighead Mark, Best Stuart, Stokes Neil R, Ratcliffe Andrew J
Abstract excerpt
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...
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