4.7 Article

Quinoxaline derivatives as herbicide safeners by improving Zea mays tolerance

Journal

PESTICIDE BIOCHEMISTRY AND PHYSIOLOGY
Volume 179, Issue -, Pages -

Publisher

ACADEMIC PRESS INC ELSEVIER SCIENCE
DOI: 10.1016/j.pestbp.2021.104958

Keywords

N,N '-disubstituted quinoxaline derivatives; Herbicide safener; Structure-activity relationship; Safener activity; Detoxification mechanism

Funding

  1. National Nature Science Foundation of China [31572042, 31801784]
  2. Natural Science Foundation of Heilongjiang Province [ZD2017002]

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The study evaluated the protective response of substituted quinoxaline derivatives on Zea mays against Isoxaflutole (IXF) toxicity, showing that most compounds displayed protection by enhancing certain activities to reduce IXF injury. Physicochemical and ADMET properties of different compounds were compared to predict pharmaceutical behavior, with safener I-6 identified as a potential candidate for developing novel safeners in the future.
Isoxaflutole (IXF), a 4-hydroxyphenylpyruvate dioxygenase (HPPD) inhibitor, causes injury to crops leading to reductions in grain yield. In order to solve the phytotoxicity caused by IXF, the present work evaluated the protective response of the substituted quinoxaline derivatives as potential safeners on Zea mays. The bioassay results showed that all of the test compounds displayed protection against IXF. In particular, safener I-6 exhibited excellent safener activity against IXF injury via enhancing glutathione (GSH) content, glutathione S transferases (GSTs) and cytochrome P450 monooxygenases (CYP450) activity. The tested compounds induced the activity of CYP450 and GSTs in Z. mays. The physicochemical properties and ADMET properties of safener I-6, benoxacor and diketonitrile (DKN, IXF metabolite) were compared to predict pharmaceutical behavior. The present work demonstrates that the safener I-6 could be considered as a potential candidate for developing novel safeners in the future.

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