2. Academic Validation
  3. Novel amino-piperidines as potent antibacterials targeting bacterial type IIA topoisomerases

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

  • Bioorg Med Chem Lett. 2011 Dec 15;21(24):7489-95. doi: 10.1016/j.bmcl.2011.09.117.
Timothy J Miles 1,  Jeffrey M Axten,  Christopher Barfoot,  Gerald Brooks,  Pamela Brown,  Dongzhao Chen,  Steven Dabbs,  David T Davies,  David L Downie,  Susanne Eyrisch,  Timothy Gallagher,  Ilaria Giordano,  Michael N Gwynn,  Alan Hennessy,  Jennifer Hoover,  Jianzhong Huang,  Graham Jones,  Roger Markwell,  William H Miller,  Elizabeth A Minthorn,  Stephen Rittenhouse,  Mark Seefeld,  Neil Pearson
Affiliations

Affiliation

  • 1 Diseases of the Developing World CEDD, GlaxoSmithKline, Calle Severo Ochoa 2, 28760, Tres Cantos, Madrid, Spain. tim.j.miles@gsk.com
PMID: 22047689 DOI: 10.1016/j.bmcl.2011.09.117
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.

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