Lipophilic teicoplanin pseudoaglycon derivatives are active against vancomycin- and teicoplanin-resistant enterococci

J Antibiot (Tokyo). 2017 May;70(5):664-670. doi: 10.1038/ja.2017.2. Epub 2017 Feb 1.

Abstract

A selection of nine derivatives of teicoplanin pseudoaglycon were tested in vitro against clinical vancomycin-resistant Enterococcus strains possessing vanA, vanB or both genes. The bacteria were characterized by PCR for the identification of their resistance genes. The tested compounds contain lipoic acid, different carbohydrates and aryl groups as lipophilic moieties. About one-third of the teicoplanin-resistant strains were shown to be susceptible to one or more of the glycopeptide derivatives.

MeSH terms

  • Anti-Bacterial Agents / chemical synthesis
  • Anti-Bacterial Agents / chemistry
  • Anti-Bacterial Agents / pharmacology*
  • Bacterial Proteins / genetics
  • Carbon-Oxygen Ligases / genetics
  • Drug Resistance, Bacterial / genetics
  • Enterococcus / drug effects*
  • Enterococcus / genetics
  • Microbial Sensitivity Tests
  • Polymerase Chain Reaction
  • Teicoplanin / chemical synthesis
  • Teicoplanin / chemistry
  • Teicoplanin / pharmacology*
  • Vancomycin / pharmacology
  • Vancomycin Resistance

Substances

  • Anti-Bacterial Agents
  • Bacterial Proteins
  • VanA ligase, Bacteria
  • VanB protein, Enterococcus
  • Teicoplanin
  • Vancomycin
  • Carbon-Oxygen Ligases