| Literature DB >> 31041863 |
Linsen Li1, Antony A Okumu1, Sheri Nolan2, Anthony English3, Sandip Vibhute1, Yanran Lu1, Katherine Hervert-Thomas4, Justin T Seffernick5, Lovette Azap1, Serena L Cole6, D Shinabarger6, Laura M Koeth7, Steffen Lindert5, Jack C Yalowich3, Daniel J Wozniak2,8, Mark J Mitton-Fry1.
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.Entities:
Keywords: gyrase; methicillin-resistant ; novel bacterial-topoisomerase inhibitors
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Year: 2019 PMID： 31041863 DOI： 10.1021/acsinfecdis.8b00375
Source DB: PubMed Journal: ACS Infect Dis ISSN： 2373-8227 Impact factor: 5.084