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Discovery and structure-activity relationships of a novel isothiazolone class of bacterial type II topoisomerase inhibitors
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- Cooper, Ian R. (author)
- Redx Pharma, Alderley Pk, Macclesfield SK10 4TG, Cheshire, England.
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- McCarroll, Andrew J. (author)
- Redx Pharma, Alderley Pk, Macclesfield SK10 4TG, Cheshire, England.
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- McGarry, David (author)
- Redx Pharma, Alderley Pk, Macclesfield SK10 4TG, Cheshire, England.
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- Redx Pharma, Alderley Pk, Macclesfield SK10 4TG, Cheshire, England Institutionen för medicinsk biokemi och mikrobiologi (creator_code:org_t)
- Elsevier BV, 2016
- 2016
- English.
- In: Bioorganic & Medicinal Chemistry Letters. - : Elsevier BV. - 0960-894X .- 1464-3405. ; 26:17, s. 4179-4183
- Journal article (peer-reviewed)
Abstract
Subject headings
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- 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.
Subject headings
- MEDICIN OCH HÄLSOVETENSKAP -- Medicinska och farmaceutiska grundvetenskaper -- Farmakologi och toxikologi (hsv//swe)
- MEDICAL AND HEALTH SCIENCES -- Basic Medicine -- Pharmacology and Toxicology (hsv//eng)
Keyword
- ESKAPE pathogens
- Anti-infectives
- Topoisomerases
- DNA gyrase
- Isothiazolone
Publication and Content Type
- ref (subject category)
- art (subject category)
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- Cooper, Ian R.
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- Forward, Henry
- Cheung, Jonathan
- Metzger, Richard
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- Nelson, Gary
- Hughes, Diarmaid
- Cao, Sha
- Maclean, John
- Charrier, Cedric
- Craighead, Mark
- Best, Stuart
- Stokes, Neil R.
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