Synthesis and Evaluation of Novel Oxyalkylated Derivatives of 2',4'-Dihydroxychalcone as Anti-Oomycete Agents against Bronopol Resistant Strains of Saprolegnia sp

Int J Mol Sci. 2016 Aug 22;17(8):1366. doi: 10.3390/ijms17081366.

Abstract

A series of novel oxyalkylchalcones substituted with alkyl groups were designed and synthesized, and the antioomycete activity of the series was evaluated in vitro against Saprolegnia strains. All tested O-alkylchalcones were synthesized by means of nucleophilic substitution from the natural compound 2',4'-dihydroxychalcone (1) and the respective alkyl bromide. The natural chalcone (1) and 10 synthetic oxyalkylchalcones (2-11) were tested against Saprolegnia parasitica and Saprolegnia australis. Among synthetic analogs, 2-hydroxy,4-farnesyloxychalcone (11) showed the most potent activity against Saprolegnia sp., with MIC and MOC values of 125 µg/mL (similar to bronopol at 150 µg/mL) and 175 µg/mL, respectively; however, 2',4'-dihydroxychalcone (1) was the strongest and most active molecule, with MIC and MOC values of 6.25 µg/mL and 12.5 µg/mL.

Keywords: Saprolegnia australis; Saprolegnia parasitica; fish pathogen; oxyalkylchalcones.

MeSH terms

  • Animals
  • Antifungal Agents / pharmacology
  • Chalcones / pharmacology*
  • Microbial Sensitivity Tests
  • Propylene Glycols / pharmacology
  • Saprolegnia / drug effects*

Substances

  • Antifungal Agents
  • Chalcones
  • Propylene Glycols
  • 2',4'-dihydroxychalcone
  • bronopol