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

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 ora...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2011-12, Vol.21 (24), p.7489-7495
Hauptverfasser:	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
Format:	Artikel
Sprache:	eng
Schlagworte:	Amino-piperidines Animals Anti-Bacterial Agents - chemistry Anti-Bacterial Agents - pharmacology Anti-Bacterial Agents - therapeutic use Antibacterial Antibacterial agents antibacterial properties Antibiotics. Antiinfectious agents. Antiparasitic agents Bacteria Bacterial type IIA topoisomerase Biological and medical sciences chemistry Dioxanes - chemistry Dioxanes - pharmacology Dioxanes - therapeutic use Disease Models, Animal DNA Topoisomerases, Type II - chemistry DNA Topoisomerases, Type II - metabolism Dogs Haplorhini Humans In vivo efficacy Lung Diseases - drug therapy Medical sciences Microbial Sensitivity Tests Naphthyridines - chemistry Naphthyridines - pharmacology Naphthyridines - therapeutic use Pharmacokinetics Pharmacology. Drug treatments Piperidines - chemistry Piperidines - pharmacology Piperidines - therapeutic use Rats Structure-Activity Relationship Topoisomerase II Inhibitors - chemistry Topoisomerase II Inhibitors - pharmacology Topoisomerase II Inhibitors - therapeutic use
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Zusammenfassung:	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.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2011.09.117