title: Structure-activity relationships of novel antibacterial translation inhibitors: 3,5-diamino-piperidinyl triazines.
abstract: Structure-activity relationships of the 3,5-diamino-piperidinyl triazine series, a novel class of bacterial translation inhibitors, are described. Optimization was focused on the triazine C-4 position in which aromatic substituents that contained electron-withdrawing groups led to potent inhibitors. The initial lack of antibacterial activity was correlated with poor cellular penetration. Whole cell antibacterial activity was achieved by linking additional aromatic moieties at the triazine C-4 position.
authors.affiliation: Anadys Pharmaceuticals, Inc., San Diego, USA.
authors.forename: Yuefen
authors.initials: Y
authors.lastname: Zhou
authors.forename: Zhongxiang
authors.initials: Z
authors.lastname: Sun
authors.forename: Jamie M
authors.initials: JM
authors.lastname: Froelich
authors.forename: Thomas
authors.initials: T
authors.lastname: Hermann
authors.forename: Daniel
authors.initials: D
authors.lastname: Wall
mesh_terms: D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D004926:Escherichia coli / Q000187:drug effects*; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D010880:Piperidines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D014176:Protein Biosynthesis / Q000187:drug effects*; D013211:Staphylococcus aureus / Q000187:drug effects*; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D014227:Triazines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D000900:Anti-Bacterial Agents; D010880:Piperidines; D014227:Triazines