Hamamelitannin Analogues that Modulate Quorum Sensing as Potentiators of Antibiotics against Staphylococcus aureus

Angew Chem Int Ed Engl. 2016 May 23;55(22):6551-5. doi: 10.1002/anie.201601973. Epub 2016 Apr 20.

Abstract

The modulation of bacterial communication to potentiate the effect of existing antimicrobial drugs is a promising alternative to the development of novel antibiotics. In the present study, we synthesized 58 analogues of hamamelitannin (HAM), a quorum sensing inhibitor and antimicrobial potentiator. These efforts resulted in the identification of an analogue that increases the susceptibility of Staphylococcus aureus towards antibiotics in vitro, in Caenorhabditis elegans, and in a mouse mammary gland infection model, without showing cytotoxicity.

Keywords: MRSA; antibiotics; biofilms; potentiators; quorum sensing.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anti-Bacterial Agents / chemistry
  • Anti-Bacterial Agents / pharmacology*
  • Dose-Response Relationship, Drug
  • Gallic Acid / analogs & derivatives*
  • Gallic Acid / chemistry
  • Gallic Acid / pharmacology
  • Hexoses / chemistry
  • Hexoses / pharmacology*
  • Microbial Sensitivity Tests
  • Molecular Structure
  • Quorum Sensing / drug effects*
  • Staphylococcus aureus / drug effects*
  • Structure-Activity Relationship

Substances

  • Anti-Bacterial Agents
  • Hexoses
  • Gallic Acid
  • hamamelitannin