Vancomycin disulfide derivatives as antibacterial agents

Bioorg Med Chem Lett. 2004 Feb 9;14(3):735-8. doi: 10.1016/j.bmcl.2003.11.040.

Abstract

A series of lipidated vancomycin analogues 1 bearing disulfide bonds within their lipid chains was designed and synthesized to optimize their ADME profiles while retaining antibacterial potency. These compounds exhibited good activity against resistant organisms and low accumulation in tissues such as kidney and liver.

Publication types

  • Comparative Study

MeSH terms

  • Animals
  • Anti-Bacterial Agents / chemical synthesis*
  • Anti-Bacterial Agents / pharmacology*
  • Disulfides* / chemical synthesis
  • Disulfides* / pharmacology
  • Drug Resistance, Microbial
  • Gram-Positive Bacteria / drug effects*
  • Kidney / drug effects*
  • Lipid Metabolism
  • Liver / drug effects*
  • Male
  • Microbial Sensitivity Tests
  • Molecular Structure
  • Rats
  • Rats, Sprague-Dawley
  • Structure-Activity Relationship
  • Vancomycin Resistance
  • Vancomycin* / analogs & derivatives
  • Vancomycin* / chemical synthesis
  • Vancomycin* / pharmacology

Substances

  • Anti-Bacterial Agents
  • Disulfides
  • Vancomycin