Novel amino-piperidines as potent antibacterials targeting bacterial type IIA topoisomerases

…, DL Downie, S Eyrisch, T Gallagher, I Giordano…

Index: 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 Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 24 p. 7489 - 7495

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Citation Number: 31

Abstract

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.