Next generation quorum sensing inhibitors: Accounts on structure activity relationship studies and biological activities

Bioorg Med Chem. 2020 Nov 1;28(21):115728. doi: 10.1016/j.bmc.2020.115728. Epub 2020 Aug 29.

Abstract

Bacterial resistance is a growing threat which represents major scourge throughout the world. The suitable way to control the present critical situation of antimicrobial resistance would be to develop entirely novel strategies to fight antibiotic resistant pathogens such as quorum sensing (QS) inhibitors or its combination with antibiotics. Anti QS agents can eliminate the QS signals and put the barrier in bio-film formation, consequently, bacterial virulence will be reduced without causing drug-resistance to the pathogens. Among the various anti QS agents identified, especially those of natural origin, furanones or acylatedhomoserine lactones (AHLs) are most popular. Semi-synthetic and synthetic inhibitors have shown greatest potential and have inspired chemists to design synthetically modified QS inhibitors with lactone moiety. This review focuses on anti QS agents (bio-film inhibitors) of both natural and synthetic origins. Further, the synthesis, structure activity relationship and anti QS activity covering literature from 2015 till March 2020 has been discussed.

Keywords: Inhibitors; Natural products; Quorum Sensing; SAR studies; Synthesis.

Publication types

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

MeSH terms

  • 4-Butyrolactone / analogs & derivatives
  • 4-Butyrolactone / chemical synthesis
  • 4-Butyrolactone / chemistry
  • 4-Butyrolactone / pharmacology
  • Anti-Bacterial Agents / chemical synthesis
  • Anti-Bacterial Agents / chemistry
  • Anti-Bacterial Agents / pharmacology*
  • Biofilms / drug effects
  • Cobalt / chemistry
  • Coordination Complexes / chemical synthesis
  • Coordination Complexes / chemistry
  • Coordination Complexes / pharmacology
  • Drug Design
  • Furans / chemistry
  • Furans / pharmacology
  • Quorum Sensing / drug effects*
  • Staphylococcus aureus / physiology
  • Structure-Activity Relationship

Substances

  • Anti-Bacterial Agents
  • Coordination Complexes
  • Furans
  • homoserine lactone
  • Cobalt
  • 4-Butyrolactone