Aug 2026· Journal of Agricultural and Food Chemistry· Vol 74 32, pp.
24949-24959
· 0 citations· 37 references
Medicine
Abstract
The application of herbicides plays a critical role in ensuring food security. However, the long-term overuse of herbicides can lead to a range of adverse effects. Therefore, it is essential to develop innovative and sustainable herbicides. A series of pyridazinone derivatives targeting phytoene desaturase (PDS) were designed and synthesized by using a structure-based drug design strategy. A bioassay showed that 16c (100%, 85%) exhibited stronger herbicidal activity against portulaca oleracea (P.o.) than that of norflurazon (NRF, 60%, 45%) in both post- and pre-emergence applications at a dosage of 150 g a.i./ha, while also showing greater safety to nontarget organisms. Meanwhile, levels of 15-cis-phytoene, carotenoids, and chlorophyll revealed that 16c effectively inhibited PDS activity. Molecular dynamics simulations and binding action assays confirmed that Arg195 is a key residue for the interaction between 16c and Synechococcus PDS (SynPDS). Therefore, 16c could be developed as a potent PDS inhibitor for herbicides.
Transketolase (TKL; EC 2.2.1.1) has been validated as a potential new herbicide target. To develop a new and highly effective herbicides-targeted TKL, a series of indole-containing fusarium acid (FA) derivatives 9a-9s were designed and synthesized. Among them, compound 9o exhibited more excellent herbicidal activity ag...
Cheng-Kun Li, Yong-Qi Liu, Xizheng Ma et al.· Journal of Agricultural and...· 0 citations
BACKGROUND
Phytopathogens have long compromised the yield and quality of crops worldwide, and the overuse of conventional synthetic pesticides has engendered a series of ecological and environmental issues. Consequently, the development of low-toxicity, high-efficacy and environmentally benign pesticides has become an...
Han Yang, Xiaoyan Pan, Dan Shen et al.· Pest Management Science· 0 citations
Enhancing innovation in herbicide discovery is imperative to combat weed resistance and safeguard global food security. To develop novel herbicide targeting dihydroorotate dehydrogenase (DHODH), a series of 3-carboxy-4-pyrazole amide lead scaffold bearing ester or acid substituents were designed and synthesized. Bioa...
Zhao-Rui Wang, Ya-Ze Li, Ji-Peng Zhang et al.· Journal of Agricultural and...· 0 citations
4-Hydroxyphenylpyruvate dioxygenase (HPPD) is an attractive target for the development of bleaching herbicides. To develop novel HPPD inhibitors, 40 diketonitrile derivatives were designed by active-fragment splicing, synthesized, and characterized. In vitro inhibitory assays against Echinochloa crus-galli HPPD (EcHPPD...
Tengfei Ma, Si-Yi Yang, Ying Bian et al.· Journal of Agricultural and...· 0 citations
Acetohydroxyacid synthase (AHAS, EC 2.2.1.6) is a core enzymatic target in agrochemical research for herbicide development and has been widely investigated in recent decades. To develop novel AHAS-targeted herbicides, twenty-three acylthiourea derivatives were synthesized via fragment recombination and bioisosteric rep...
Bin-Bin Jiang, Xi-Ying Chen, Xu-Biao He et al.· Molecules· 0 citations
BACKGROUND
Agricultural pests significantly reduce crop yields and threaten global food security. Chemical pesticides remain the primary means of pest control. In this study, celangulin V, a plant-derived insecticide, was used as a lead compound. Guided by three-dimensional quantitative structure-activity relationship...
Zi-Yu Wang, Yuan-Yuan Yang, Rong Tang et al.· Pest Management Science· 0 citations
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