Splicing Indoles and 4,5-Dihydro-1 H-pyrazoline Structure Gave Birth to Novel Antiviral Agents: Design, Synthesis, and Mechanism Study

J Agric Food Chem. 2023 May 17;71(19):7239-7249. doi: 10.1021/acs.jafc.3c01005. Epub 2023 May 9.

Abstract

The specific conation of our research is to invent a series of indole derivatives containing a 4,5-dihydro-1H-pyrazoline motif with effective antiviral activity. The anti-potato virus Y (PVY) activities of target compounds were systematically investigated. Most target compounds exhibited good PVY activities. Compound D40, which exhibited outstanding anti-PVY activities, was sieved using a three-dimensional quantitative structure-activity relationship. Based on the anti-PVY activity assessments, the curative and protective activities of D40 were found to be 64.9 and 60.8%, respectively, which were superior to those of the commercial drug Ningnanmycin (50.2 and 50.7%, respectively). In addition, defensive enzyme activities and proteomics results indicate that D40 can increase the three crucial defense-related enzyme activities and regulate the carbon fixation pathway in photosynthetic organisms to intensify the resistance of plants to PVY. Therefore, our study suggests that compound D40 might be used as a suitable crop protection pesticide.

Keywords: 3D-QSAR; 4,5-dihydro-1H-pyrazoline; indole derivatives; potato virus Y; proteomics.

MeSH terms

  • Antiviral Agents / chemistry
  • Drug Design
  • Indoles / chemistry
  • Indoles / pharmacology
  • Plant Diseases / prevention & control
  • Potyvirus*
  • Quantitative Structure-Activity Relationship
  • Tobacco Mosaic Virus*

Substances

  • Antiviral Agents
  • Indoles