title: Novel amino-piperidines as potent antibacterials targeting bacterial type IIA topoisomerases.
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.
authors: Diseases of the Developing World CEDD, GlaxoSmithKline, Calle Severo Ochoa 2, 28760, Tres Cantos, Madrid, Spain. tim.j.miles@gsk.com
authors: Timothy J
authors: TJ
authors: Miles
authors: Jeffrey M
authors: JM
authors: Axten
authors: Christopher
authors: C
authors: Barfoot
authors: Gerald
authors: G
authors: Brooks
authors: Pamela
authors: P
authors: Brown
authors: Dongzhao
authors: D
authors: Chen
authors: Steven
authors: S
authors: Dabbs
authors: David T
authors: DT
authors: Davies
authors: David L
authors: DL
authors: Downie
authors: Susanne
authors: S
authors: Eyrisch
authors: Timothy
authors: T
authors: Gallagher
authors: Ilaria
authors: I
authors: Giordano
authors: Michael N
authors: MN
authors: Gwynn
authors: Alan
authors: A
authors: Hennessy
authors: Jennifer
authors: J
authors: Hoover
authors: Jianzhong
authors: J
authors: Huang
authors: Graham
authors: G
authors: Jones
authors: Roger
authors: R
authors: Markwell
authors: William H
authors: WH
authors: Miller
authors: Elizabeth A
authors: EA
authors: Minthorn
authors: Stephen
authors: S
authors: Rittenhouse
authors: Mark
authors: M
authors: Seefeld
authors: Neil
authors: N
authors: Pearson
mesh_terms: D000818:Animals; D000900:Anti-Bacterial Agents / Q000737:chemistry* / Q000494:pharmacology* / Q000627:therapeutic use; D004250:DNA Topoisomerases, Type II / Q000737:chemistry* / Q000378:metabolism; D004146:Dioxanes / Q000737:chemistry* / Q000494:pharmacology* / Q000627:therapeutic use; D004195:Disease Models, Animal; D004285:Dogs; D000882:Haplorhini; D006801:Humans; D008171:Lung Diseases / Q000188:drug therapy; D008826:Microbial Sensitivity Tests; D009287:Naphthyridines / Q000737:chemistry* / Q000494:pharmacology* / Q000627:therapeutic use; D010880:Piperidines / Q000737:chemistry* / Q000494:pharmacology / Q000627:therapeutic use; D051381:Rats; D013329:Structure-Activity Relationship; D059005:Topoisomerase II Inhibitors / Q000737:chemistry* / Q000494:pharmacology / Q000627:therapeutic use
chemical_list: D000900:Anti-Bacterial Agents; D004146:Dioxanes; D009287:Naphthyridines; D010880:Piperidines; D059005:Topoisomerase II Inhibitors; D004250:DNA Topoisomerases, Type II