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Novel hydroxyl tricyclics (e.g., GSK966587) as potent inhibitors of bacterial type IIA topoisomerases

Miles, Timothy J., Hennessy, Alan J., Bax, Ben ORCID:, Brooks, Gerald, Brown, Barry S., Brown, Pamela, Cailleau, Nathalie, Chen, Dongzhao, Dabbs, Steven, Davies, David T., Esken, Joel M., Giordano, Ilaria, Hoover, Jennifer L., Huang, Jianzhong, Jones, Graham E., Kusalakumari Sukmar, Senthill K., Spitzfaden, Claus, Markwell, Roger E., Minthorn, Elisabeth A., Rittenhouse, Steve, Gwynn, Michael N. and Pearson, Neil D. 2013. Novel hydroxyl tricyclics (e.g., GSK966587) as potent inhibitors of bacterial type IIA topoisomerases. Bioorganic and Medicinal Chemistry Letters 23 (19) , pp. 5437-5441. 10.1016/j.bmcl.2013.07.013

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During the course of our research to find novel mode of action antibacterials, we discovered a series of hydroxyl tricyclic compounds that showed good potency against Gram-positive and Gram-negative pathogens. These compounds inhibit bacterial type IIA topoisomerases. Herein we will discuss structure–activity relationships in this series and report advanced studies on compound 1 (GSK966587) which demonstrates good PK and in vivo efficacy properties. X-ray crystallographic studies were used to provide insight into the structural basis for the difference in antibacterial potency between enantiomers.

Item Type: Article
Date Type: Publication
Status: Published
Schools: Biosciences
Publisher: Elsevier
ISSN: 0960-894X
Date of Acceptance: 9 July 2013
Last Modified: 23 Oct 2022 14:03

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