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Novel amino-piperidines as potent antibacterials targeting bacterial type IIA topoisomerases |
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| Authors: | 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 |
| Institution: | aDiseases of the Developing World CEDD, GlaxoSmithKline, Calle Severo Ochoa 2, 28760, Tres Cantos, Madrid, Spain;bInfectious Diseases CEDD, GlaxoSmithKline, Gunnels Wood Road, Stevenage SG1 2NY, UK;cInfectious Diseases CEDD, GlaxoSmithKline, Third Avenue, Harlow CM19 5AW, UK;dInfectious Diseases CEDD, GlaxoSmithKline, 1250 South Collegeville Road, Collegeville, PA 19426, USA;eBiological Reagents & Assay Development, GlaxoSmithKline, Gunnels Wood Road, Stevenage SG1 2NY, UK |
| 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. |
| Keywords: | Antibacterial Bacterial type IIA topoisomerase Amino-piperidines Pharmacokinetics In vivo efficacy |
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