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Discovery and structure-activity relationships of a novel isothiazolone class of bacterial type II topoisomerase inhibitors
Redx Pharma, Alderley Pk, Macclesfield SK10 4TG, Cheshire, England..
Redx Pharma, Alderley Pk, Macclesfield SK10 4TG, Cheshire, England..
Redx Pharma, Alderley Pk, Macclesfield SK10 4TG, Cheshire, England..
Redx Pharma, Alderley Pk, Macclesfield SK10 4TG, Cheshire, England..
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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
Abstract [en]

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.
Keyword [en]
ESKAPE pathogens, Anti-infectives, Topoisomerases, DNA gyrase, Isothiazolone
National Category
Pharmacology and Toxicology
Identifiers
URN: urn:nbn:se:uu:diva-303258DOI: 10.1016/j.bmcl.2016.07.061ISI: 000381959900005PubMedID: 27499455OAI: oai:DiVA.org:uu-303258DiVA: diva2:971490
Funder
EU, FP7, Seventh Framework Programme, 115583
Available from: 2016-09-16 Created: 2016-09-15 Last updated: 2016-09-16Bibliographically approved

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Hughes, DiarmaidCao, Sha
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Department of Medical Biochemistry and Microbiology
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