Biofilm inhibition and anti-Candida activity of a cationic lipo-benzamide molecule with twin-nonyl chain

Bioorg Med Chem Lett. 2018 Jun 1;28(10):1776-1780. doi: 10.1016/j.bmcl.2018.04.024. Epub 2018 Apr 12.

Abstract

A series of cationic lipo-benzamide compounds with varying lengths of hydrocarbon chains (C2M-C18M) were evaluated for anti-Candida activity. Four compounds harbouring 8-11 hydrocarbon chains demonstrated concentration-dependent inhibition of fungal cell growth with Minimum Inhibitory Concentration (MIC) of ≤6.2 µg ml-1. The most active compound (C9M) inhibited growth of both Candida albicans and non-albicans strains and is equally active against pairs of azole sensitive and resistant clinical isolates of C. albicans. Compound C9M also inhibited different stages of Candida biofilms. Scanning Electron Microscopy (SEM) of Candida cells after C9M treatment was also done and no significant cell lysis was observed. Hemolysis assay was performed and only 2.5% haemolysis was observed at MIC concentration.

Keywords: Antifungal activity; Biofilm; Candida albicans; Cationic lipo-benzamide; Multi drug resistance.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Alkanes / chemistry
  • Alkanes / pharmacology*
  • Antifungal Agents / chemical synthesis
  • Antifungal Agents / chemistry
  • Antifungal Agents / pharmacology*
  • Benzamides / chemical synthesis
  • Benzamides / chemistry
  • Benzamides / pharmacology
  • Biofilms / drug effects*
  • Candida albicans / cytology
  • Candida albicans / drug effects*
  • Cations / chemical synthesis
  • Cations / chemistry
  • Cations / pharmacology
  • Cell Line
  • Cell Survival / drug effects
  • Dose-Response Relationship, Drug
  • Humans
  • Microbial Sensitivity Tests
  • Molecular Structure
  • Structure-Activity Relationship

Substances

  • Alkanes
  • Antifungal Agents
  • Benzamides
  • Cations
  • benzamide
  • nonane