title: Synthesis and SAR of 3,5-diamino-piperidine derivatives: novel antibacterial translation inhibitors as aminoglycoside mimetics.
abstract: Aminoglycoside antibiotics target an internal RNA loop within the bacterial ribosomal decoding site. Here, we describe the synthesis and SAR of novel 3,5-diamino-piperidine derivatives as aminoglycoside mimetics, and show they act as inhibitors of bacterial translation and growth.
authors.affiliation: Anadys Pharmaceuticals, Inc., San Diego, CA 92121, USA.
authors.forename: Yuefen
authors.initials: Y
authors.lastname: Zhou
authors.forename: Vlad E
authors.initials: VE
authors.lastname: Gregor
authors.forename: Benjamin K
authors.initials: BK
authors.lastname: Ayida
authors.forename: Geoffrey C
authors.initials: GC
authors.lastname: Winters
authors.forename: Zhongxiang
authors.initials: Z
authors.lastname: Sun
authors.forename: Douglas
authors.initials: D
authors.lastname: Murphy
authors.forename: Greg
authors.initials: G
authors.lastname: Haley
authors.forename: Dwight
authors.initials: D
authors.lastname: Bailey
authors.forename: Jamie M
authors.initials: JM
authors.lastname: Froelich
authors.forename: Sarah
authors.initials: S
authors.lastname: Fish
authors.forename: Stephen E
authors.initials: SE
authors.lastname: Webber
authors.forename: Thomas
authors.initials: T
authors.lastname: Hermann
authors.forename: Daniel
authors.initials: D
authors.lastname: Wall
mesh_terms: D000617:Aminoglycosides; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D018716:Molecular Mimicry; D010880:Piperidines / Q000138:chemical synthesis* / Q000494:pharmacology*; D014176:Protein Biosynthesis / Q000187:drug effects; D011550:Pseudomonas aeruginosa / Q000187:drug effects / Q000235:genetics / Q000254:growth & development; D013329:Structure-Activity Relationship
chemical_list: D000617:Aminoglycosides; D000900:Anti-Bacterial Agents; D010880:Piperidines