2. Academic Validation
  3. Pesticidal evaluation of novel dual-chiral N-cyano sulfiliminyl anthranilic diamides derivatives

Pesticidal evaluation of novel dual-chiral N-cyano sulfiliminyl anthranilic diamides derivatives

  • J Enzyme Inhib Med Chem. 2026 Dec;41(1):2627052. doi: 10.1080/14756366.2026.2627052.
Xiaomin Li 1,  Mukuo Wang 2,  Shuying Li 1,  Weibin Xie 3,  Ruyi Jin 4,  Yongtao Xie 3,  Shaa Zhou 5,  Lixia Xiong 3,  Na Yang 3,  Sha Zhou 3
Affiliations

Affiliations

  • 1 State Key Laboratory of Medicinal Chemical Biology, Nankai University, Tianjin, People's Republic of China.
  • 2 College of Pharmacy and Tianjin Key Laboratory of Molecular Drug Research, State Key Laboratory of Medicinal Chemical Biology, Nankai University, Tianjin, China.
  • 3 College of Chemistry, National Pesticidal Engineering Centre (Tianjin), State Key Laboratory of Elemento-Organic Chemistry, Institute of Elemento-Organic Chemistry, Nankai University, Tianjin, China.
  • 4 College of Pharmacy, Shaanxi University of Chinese Medicine, Xi'an, China.
  • 5 School of Forestry and Biotechnology, Collaborative Innovation Center of Green Pesticide, National Joint Engineering Laboratory of Biopesticide Preparation, Zhejiang A&F University, Hangzhou, China.
PMID: 41712261 DOI: 10.1080/14756366.2026.2627052
Abstract

To develop eco-friendly pesticides with novel modes of action for insect management, a series of dual-chiral N-cyano sulfilimine-substituted anthranilic diamides were designed and synthesised de novo, and their insecticidal activities were evaluated against Mythimna separata (M. separata) and Plutella xylostella (P. xylostella). Most target compounds exhibited potent insecticidal activity against M. separata. Notably, compounds 6a-b and 6f-g demonstrated near-complete inhibition at 0.1 mg/L, achieving efficacy comparable to the commercial standard chlorantraniliprole (CHL). Furthermore, 6g and 7h outperformed CHL against P. xylostella, suggesting enhanced specificity. 6g matchedCHL's efficacy against M. separata. Specific target compounds, including 6g and 7h, emerged as potential modulators of insect ryanodine receptor (RyR). Molecular docking revealed that 6g probably formed three hydrogen bonds with RyR binding pocket and exhibited stronger binding affinity than CHL (two hydrogen bonds). These findings provide a structural foundation for rational design of novel chiral sulfiliminyl RyR-targeting insecticides.

Keywords

Ryanodine receptor; anthranilic diamides; dual-chiral; insecticidal activity; sulfilimines.

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