Synthesis and SAR of 3,5-diamino-piperidine derivatives: novel antibacterial translation inhibitors as aminoglycoside mimetics

Bioorg Med Chem Lett. 2007 Mar 1;17(5):1206-10. doi: 10.1016/j.bmcl.2006.12.024. Epub 2006 Dec 12.

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.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Aminoglycosides
  • Anti-Bacterial Agents / chemical synthesis*
  • Anti-Bacterial Agents / pharmacology
  • Molecular Mimicry
  • Piperidines / chemical synthesis*
  • Piperidines / pharmacology*
  • Protein Biosynthesis / drug effects
  • Pseudomonas aeruginosa / drug effects
  • Pseudomonas aeruginosa / genetics
  • Pseudomonas aeruginosa / growth & development
  • Structure-Activity Relationship

Substances

  • Aminoglycosides
  • Anti-Bacterial Agents
  • Piperidines