Related Experiment Video
Updated: Jun 3, 2026

Microwave-Assisted Preparation of 1-Aryl-1H-pyrazole-5-amines
Published on: June 23, 2019
From Rational Design to Bioactivity Enhancement: Novel Benzofuranone Insecticide Discovery Assisted by a
Renxuan Zou1,2, Jinyang Zhou1,2, Ziyan Yang1,2
1Innovation Center of Pesticide Research, Department of Applied Chemistry, College of Science, China Agricultural University, Beijing 100193, People's Republic of China.
Abstract:
Developing novel-structured insecticidal agents targeting nAChR has become increasingly urgent. In this work, novel benzofuranone compounds were designed and synthesized, whose mortality rates against Myzus persicae and Aphis glycines were 30-80%. Compound 5i exhibited the best bioactivities (LC50 = 106.86 and 43.94 μg/mL against M. persicae and A. glycines, respectively) due to its π-π interactions with key residues (TRP143 and TYR186). To further enhance the insecticidal efficacy of compound 5i, calix[4]arene (C4A) was applied to improve its solubility through the supramolecular host-guest complex C4A@5i. The insecticidal activities of C4A@5i were effectively enhanced against M. persicae (LC50 = 56.66 μg/mL) and A. glycines (LC50 = 26.98 μg/mL). The enhanced solubility of compound 5i (6.27-fold) was the reason for the improved insecticidal activities of C4A@5i. Besides, compound 5i, C4A, and C4A@5i showed low bee toxicity. This study provides guidance for novel benzofuranone compounds as insecticidal candidates and serves as a reference for the development of ecologically safe supramolecular insecticides.
Related Concept Videos
Structure-Activity Relationships and Drug Design
SAR studies the intricate relationship between a drug's chemical structure and biological activity. It focuses on understanding how modifications to a drug's structure can influence its...
Electrophilic Aromatic Substitution: Fluorination and Iodination of Benzene
Nucleophilic Aromatic Substitution: Elimination–Addition
Diazonium Group Substitution with Halogens and Cyanide: Sandmeyer and Schiemann Reactions
Benzene to 1,4-Cyclohexadiene: Birch Reduction Mechanism
