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
  • 1. Diseases of the Developing World CEDD, GlaxoSmithKline, Calle Severo Ochoa 2, 28760, Tres Cantos, Madrid, Spain. [email protected]
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.