New Thiazole Nortopsentin Analogues Inhibit Bacterial Biofilm Formation

Mar Drugs. 2018 Aug 4;16(8):274. doi: 10.3390/md16080274.

Abstract

New thiazole nortopsentin analogues were conveniently synthesized and evaluated for their activity as inhibitors of biofilm formation of relevant Gram-positive and Gram-negative pathogens. All compounds were able to interfere with the first step of biofilm formation in a dose-dependent manner, showing a selectivity against the staphylococcal strains. The most active derivatives elicited IC50 values against Staphylococcus aureus ATCC 25923, ranging from 0.40⁻2.03 µM. The new compounds showed a typical anti-virulence profile, being able to inhibit the biofilm formation without affecting the microbial growth in the planktonic form.

Keywords: anti-virulence agents; antibiofilm agents; marine alkaloids; nortopsentin analogues; thiazole derivatives.

MeSH terms

  • Anti-Bacterial Agents / chemical synthesis
  • Anti-Bacterial Agents / pharmacology*
  • Aquatic Organisms / chemistry
  • Biofilms / drug effects*
  • Drug Resistance, Bacterial*
  • Humans
  • Imidazoles / chemistry
  • Indoles / chemistry
  • Inhibitory Concentration 50
  • Staphylococcal Infections / drug therapy
  • Staphylococcal Infections / microbiology
  • Staphylococcal Infections / pathology
  • Staphylococcus aureus / drug effects
  • Staphylococcus aureus / physiology
  • Thiazoles / chemical synthesis
  • Thiazoles / pharmacology*

Substances

  • Anti-Bacterial Agents
  • Imidazoles
  • Indoles
  • Thiazoles
  • topsentin A