Chemistry Faculty Work
Title
1,3-Dioxane-Linked Bacterial Topoisomerase Inhibitors with Enhanced Antibacterial Activity and Reduced hERG Inhibition
Document Type
Article
Publication Date
2019
Publication Title
ACS Infectious Diseases
Volume Number
5
Issue Number
7
DOI
10.1021/acsinfecdis.8b00375
Abstract
The development of new therapies to treat methicillin-resistant Staphylococcus aureus (MRSA) is needed to counteract the significant threat that MRSA presents to human health. Novel inhibitors of DNA gyrase and topoisomerase IV (TopoIV) constitute one highly promising approach, but continued optimization is required to realize the full potential of this class of antibiotics. Herein, we report further studies on a series of dioxane-linked derivatives, demonstrating improved antistaphylococcal activity and reduced hERG inhibition. A subseries of analogues also possesses enhanced inhibition of the secondary target, TopoIV.
ISSN
2373-8227
First Page
1115
Last Page
1128
Recommended Citation
Hervert, Katherine; Li, Linsen; Okumu, Antony A.; Nolan, Sheri; English, Anthony; Vibhute, Sandip; and Lu, Yanran, "1,3-Dioxane-Linked Bacterial Topoisomerase Inhibitors with Enhanced Antibacterial Activity and Reduced hERG Inhibition" (2019). Chemistry Faculty Work. 17.
https://digitalcommons.owu.edu/chem_pubs/17
Link Out URL
https://doi.org/10.1021/acsinfecdis.8b00375