Development of celecoxib-derived antifungals for crop protection

Bioorg Chem. 2020 Apr:97:103670. doi: 10.1016/j.bioorg.2020.103670. Epub 2020 Feb 15.

Abstract

Selective COX-2 inhibitor celecoxib was found directly inhibiting the growth of tested phytopathogenic fungi with the inhibitory rate ranging from 30 to 40% at 100 µg/ml. Lead optimization of celecoxib led to the identification of compound 12 among its derivatives as the most active antifungal candidate. The antifungal effect of compound 12 was supposed to be independent of COX-2 inhibition. Transcriptome profiling analysis of Fusarium graminearium (PH-1) treated with compound 12 brought about 406 up-regulated and 572 down-regulated differentially express genes (DEGs) respectively.

Keywords: Antifungal agrochemical; COX-2 inhibitor; Celecoxib; Lead optimization.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Celecoxib / analogs & derivatives*
  • Celecoxib / toxicity
  • Crop Protection / methods*
  • Crops, Agricultural / microbiology
  • Cyclooxygenase 2 Inhibitors / chemistry*
  • Cyclooxygenase 2 Inhibitors / toxicity
  • Fungicides, Industrial / chemistry*
  • Fungicides, Industrial / toxicity
  • Fusarium / drug effects*
  • Fusarium / genetics
  • Gene Expression Regulation, Fungal / drug effects
  • Plant Diseases / microbiology
  • Plant Diseases / prevention & control*
  • Transcriptome / drug effects

Substances

  • Cyclooxygenase 2 Inhibitors
  • Fungicides, Industrial
  • Celecoxib

Supplementary concepts

  • Fusarium graminearum