Discovery and structure-activity relationships of a novel isothiazolone class of bacterial type II topoisomerase inhibitors
2016 (English)In: Bioorganic & Medicinal Chemistry Letters, ISSN 0960-894X, E-ISSN 1090-2120, Vol. 26, no 17, 4179-4183 p.Article in journal (Refereed) Published
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.
Place, publisher, year, edition, pages
2016. Vol. 26, no 17, 4179-4183 p.
ESKAPE pathogens, Anti-infectives, Topoisomerases, DNA gyrase, Isothiazolone
Pharmacology and Toxicology
IdentifiersURN: urn:nbn:se:uu:diva-303258DOI: 10.1016/j.bmcl.2016.07.061ISI: 000381959900005PubMedID: 27499455OAI: oai:DiVA.org:uu-303258DiVA: diva2:971490
FunderEU, FP7, Seventh Framework Programme, 115583