Novel amino-piperidines as potent antibacterials targeting bacterial type IIA topoisomerases
2011
Miles, Timothy J. | Axten, Jeffrey M. | Barfoot, Christopher | Brooks, Gerald | Brown, Pamela | Chen, Dongzhao | Dabbs, Steven | Davies, David T. | Downie, David L. | Eyrisch, Susanne | Gallagher, Timothy | Giordano, Ilaria | Gwynn, Michael N. | Hennessy, Alan | Hoover, Jennifer | Huang, Jianzhong | Jones, Graham | Markwell, Roger | Miller, William H. | Minthorn, Elizabeth A. | Rittenhouse, Stephen | Seefeld, Mark | Pearson, Neil
We have identified a series of amino-piperidine antibacterials with a good broad spectrum potency. We report the investigation of various subunits in this series and advanced studies on compound 8. Compound 8 possesses good pharmacokinetics, broad spectrum antibacterial activity and demonstrates oral efficacy in a rat lung infection model.
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