Miles, Timothy J., Hennessy, Alan J., Bax, Ben ORCID: https://orcid.org/0000-0003-1940-3785, 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 |
Official URL: http://dx.doi.org/10.1016/j.bmcl.2016.03.106
Abstract
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 |
URI: | https://orca.cardiff.ac.uk/id/eprint/111250 |
Citation Data
Cited 35 times in Scopus. View in Scopus. Powered By Scopus® Data
Actions (repository staff only)
Edit Item |