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  2. A Novel AHAS-Inhibiting Herbicide Candidate for Controlling Leptochloa chinensis: A Devastating Weedy Grass in Rice Fields

A Novel AHAS-Inhibiting Herbicide Candidate for Controlling Leptochloa chinensis: A Devastating Weedy Grass in Rice Fields

  • J Agric Food Chem. 2024 Jul 24;72(29):16140-16151. doi: 10.1021/acs.jafc.4c03891.
Yinglu Chen 1 Yitao Yan 1 Jie Chen 2 Ben Zheng 3 Youwei Jiang 3 Zhengzhong Kang 4 Jun Wu 1
Affiliations

Affiliations

  • 1 Department of Chemistry, Zhejiang University, Hangzhou 310058, China.
  • 2 National Joint Local Engineering Laboratory for High-Efficient Preparation of Biopesticide, College of Forestry and Biotechnology, Zhejiang A & F University, Hangzhou 311300, China.
  • 3 Hangzhou Jingyinkang Biological Technology Co., Ltd., Hangzhou 311110, China.
  • 4 Beijing Life Science Academy, Beijing 102200, China.
Abstract

Given the prevalence of the malignant weed Chinese Sprangletop (Leptochloa chinensis (L.) Nees) in rice fields, the development of novel herbicides against this weed has aroused wide interest. Here, we report a novel diphenyl ether-pyrimidine hybrid, DEP-5, serving as a systematic pre/postemergence herbicide candidate for broad-spectrum weed control in rice fields, specifically for L. chinensis. Notably, DEP-5 exhibits over 80% herbicidal activity against the resistant biotypes even at 37.5 g a.i./ha under greenhouse conditions and has complete control of L. chinensis at 150 g a.i./ha in the rice fields. We uncover that DEP-5 acts as a noncompetitive inhibitor of acetohydroxyacid synthase (AHAS) with an inhibition constant (Ki) of 39.4 μM. We propose that DEP-5 binds to AHAS in two hydrophobic-driven binding modes that differ from commercial AHAS inhibitors. Overall, these findings demonstrate that DEP-5 has great potential to be developed into a herbicide for L. chinensis control and inspire fresh concepts for novel AHAS-inhibiting herbicide design.

Keywords

AHAS; SAACS; diphenyl ether; docking; herbicide; hydrophobic interaction; resistant L. chinensis; rice field.

Figures
Products
  • Cat. No.
    Product Name
    Description
    Target
    Research Area
  • HY-162691
    AHAS 抑制剂