Design, synthesis and antifungal activity of novel furancarboxamide derivatives

Eur J Med Chem. 2016 Sep 14:120:244-51. doi: 10.1016/j.ejmech.2016.04.060. Epub 2016 Apr 26.

Abstract

Twenty-seven novel furancarboxamide derivatives with a diphenyl ether moiety were synthesized and evaluated for their antifungal activity against Rhizoctonia solani, Botrytis cirerea, Valsa mali and Sphaceloma ampelimum. Antifungal bioassay results indicated that most compounds had good or excellent fungicidal activities for R. solani and S. ampelimum at 20 mg L(-1). Among synthesized compounds, compound 18e showed a greater inhibitory effect against S. ampelimum, with half maximal effective concentration (EC50) values of 0.020 mg L(-1). This strong activity rivals currently used commercial fungicides, such as Boscalid and Carbendazim, and has great potential as a lead compound for future development of novel fungicides.

Keywords: Antifungal activity; Diphenyl ether; Furancarboxamides; Synthesis.

MeSH terms

  • Antifungal Agents / chemical synthesis*
  • Antifungal Agents / pharmacology
  • Drug Design
  • Furans / chemistry
  • Furans / pharmacology*
  • Microbial Sensitivity Tests
  • Microbial Viability
  • Structure-Activity Relationship

Substances

  • Antifungal Agents
  • Furans