Synthesis and SAR of 3,5-diamino-piperidine derivatives: novel antibacterial translation inhibitors as aminoglycoside mimetics.
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.
Zhou
Yuefen
Y
Anadys Pharmaceuticals, Inc., San Diego, CA 92121, USA.
Gregor
Vlad E
VE
Ayida
Benjamin K
BK
Winters
Geoffrey C
GC
Sun
Zhongxiang
Z
Murphy
Douglas
D
Haley
Greg
G
Bailey
Dwight
D
Froelich
Jamie M
JM
Fish
Sarah
S
Webber
Stephen E
SE
Hermann
Thomas
T
Wall
Daniel
D
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
D000617:Aminoglycosides; D000900:Anti-Bacterial Agents; D010880:Piperidines