724788-70-9Relevant articles and documents
1,3-Dioxane-Linked Bacterial Topoisomerase Inhibitors with Enhanced Antibacterial Activity and Reduced hERG Inhibition
Li, Linsen,Okumu, Antony A.,Nolan, Sheri,English, Anthony,Vibhute, Sandip,Lu, Yanran,Hervert-Thomas, Katherine,Seffernick, Justin T.,Azap, Lovette,Cole, Serena L.,Shinabarger,Koeth, Laura M.,Lindert, Steffen,Yalowich, Jack C.,Wozniak, Daniel J.,Mitton-Fry, Mark J.
, p. 1115 - 1128 (2019)
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.
TYPE II TOPOISOMERASE INHIBITORS AND METHODS OF MAKING AND USING THEREOF
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Page/Page column 73, (2018/11/22)
Disclosed are Type II Topoisomerase Inhibitors, analogs thereof, pharmaceutical compositions thereof, and methods of making and using these compounds and compositions. Methods of using the disclosed compounds to treat infections, such as MRSA, MDR P. aeruginosa, and other pathogens are also described.
Oxabicyclooctane-linked novel bacterial topoisomerase inhibitors as broad spectrum antibacterial agents
Singh, Sheo B.,Kaelin, David E.,Wu, Jin,Miesel, Lynn,Tan, Christopher M.,Meinke, Peter T.,Olsen, David,Lagrutta, Armando,Bradley, Prudence,Lu, Jun,Patel, Sangita,Rickert, Keith W.,Smith, Robert F.,Soisson, Stephen,Wei, Changqing,Fukuda, Hideyuki,Kishii, Ryuta,Takei, Masaya,Fukuda, Yasumichi
supporting information, p. 609 - 614 (2014/06/09)
Bacterial resistance is eroding the clinical utility of existing antibiotics necessitating the discovery of new agents. Bacterial type II topoisomerase is a clinically validated, highly effective, and proven drug target. This target is amenable to inhibit