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Synthesis and anti-staphylococcal activity of novel bacterial topoisomerase inhibitors with a 5-amino-1,3-dioxane linker moiety |
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| Authors: | Linsen Li Antony Okumu Sheri Dellos-Nolan Zoe Li Soumendrakrishna Karmahapatra Anthony English Jack C. Yalowich Daniel J. Wozniak Mark J. Mitton-Fry |
| Affiliation: | 1. Division of Medicinal Chemistry and Pharmacognosy, The Ohio State University, Columbus, OH 43210, USA;2. Microbial Infection and Immunity, The Ohio State University, Columbus, OH 43210, USA;3. Division of Pharmacology, The Ohio State University, Columbus, OH 43210, USA;4. Department of Microbiology, The Ohio State University, Columbus, OH 43210, USA |
| Abstract: | Novel bacterial type II topoisomerase inhibitors (NBTIs) constitute a promising new class of antibacterial agents. We report a series of NBTIs with potent anti-staphylococcal activity and diminished hERG inhibition. Dioxane-linked compound 9 demonstrated MICs ≤1?μg/mL against both methicillin-susceptible (MSSA) and -resistant Staphylococcus aureus (MRSA), accompanied by reduced hERG inhibition as compared to cyclohexane- or piperidine-linked analogs. |
| Keywords: | MRSA NBTI Gyrase Topoisomerase TopoIV Antibacterial |
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