Development of quinoline-based disruptors of biofilm formation against Vibrio cholerae

Org Lett. 2013 Mar 15;15(6):1234-7. doi: 10.1021/ol400150z. Epub 2013 Mar 5.

Abstract

Biofilm formation is a major cause of bacterial persistence in nosocomial infections, leading to extended treatment times and increased rates of morbidity and mortality. Despite this, there are currently no biofilm inhibitors approved for clinical use. The synthesis and biological evaluation of a library of amino alcohol quinolines as lead compounds for the disruption of biofilm formation in Vibrio cholerae is now reported. Application of selective metal-halogen exchange chemistry installed both stereocenters in one step, to afford a simpler scaffold than the initial lead molecule, with an EC50 < 10 μM.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, Non-P.H.S.

MeSH terms

  • Biofilms / drug effects*
  • Biofilms / growth & development
  • Combinatorial Chemistry Techniques
  • Cross Infection / drug therapy
  • Cross Infection / microbiology
  • Microscopy, Confocal
  • Molecular Structure
  • Quinolines / chemical synthesis*
  • Quinolines / chemistry
  • Quinolines / therapeutic use
  • Vibrio cholerae / drug effects
  • Vibrio cholerae / growth & development
  • Vibrio cholerae / physiology*

Substances

  • Quinolines