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Novel tricyclics (e.g., GSK945237) 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., Jones, Graham E., Kusalakumari Sukmar, Senthill K., Markwell, Roger E., Minthorn, Elisabeth A., Rittenhouse, Steve, Gwynn, Michael N. and Pearson, Neil D. 2016. Novel tricyclics (e.g., GSK945237) as potent inhibitors of bacterial type IIA topoisomerases. Bioorganic and Medicinal Chemistry Letters 26 (10) , pp. 2464-2469. 10.1016/j.bmcl.2016.03.106

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During the course of our research on the lead optimisation of the NBTI (Novel Bacterial Type II Topoisomerase Inhibitors) class of antibacterials, we discovered a series of tricyclic compounds that showed good Gram-positive and Gram-negative potency. Herein we will discuss the various subunits that were investigated in this series and report advanced studies on compound 1 (GSK945237) which demonstrates good PK and in vivo efficacy properties.

Item Type: Article
Date Type: Publication
Status: Published
Schools: Biosciences
Publisher: Elsevier
ISSN: 0960-894X
Date of First Compliant Deposit: 8 May 2018
Date of Acceptance: 29 March 2016
Last Modified: 23 Oct 2022 13:38

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