Advanced Agrochem最新文献

4-Hydroxyphenylpyruvate dioxygenase (EC 1.13.11.27, HPPD) is currently one of the popular targets of herbicide research, and herbicides targeting it have shown promising results in treating resistant weeds. However, the long-term application of HPPD inhibitors with in their classical scaffolds inevitably leads to the development of drug resistance. To further delay the underlying development of weed resistance to HPPD inhibitors, we successfully screened HPPD inhibitor pharmacophore with novel chelate structures using computer-aided drug molecular design and obtained 2-trifluoromethyltetrazolium nicotinamide derivatives through active fragment splicing. Among these derivatives, 6-(3,3-diethyl-1-methylureido)-N-(1-methyl-1H-tetrazol-5-yl)-2-(trifluoromethyl)nicotinamide (compound 31), exhibited the most promising in vitro enzyme inhibitory activity, with IC₅₀ value of 0.072 μM, which was approximately five times better than that of the control agent mesotrione (IC₅₀ = 0.363 μM). The crystal structure of the AtHPPD complexed with compound 31 (2.0 Å) and the binding energy calculations of the representative compounds revealed several important interactions of the ligand binding to the target protein, which explained the superior enzyme inhibitory activity of the compounds at the molecular level. In addition, compounds 7 and 31 possessed 100% inhibition against the five target weeds at the tested dosage and both were more effective against Setaria viridis than mesotrione. In general, it is promising to design novel HPPD inhibitors by developing novel chelating structures, and compounds 7 or 31 could be used as the leads for further development of valuable HPPD inhibitors.

Agricultural chemicals with multifunctional applications in crop protection have attracted increasing attention. Herein, two new series of thiazole and imidazo[1,2-a]pyridine derivatives containing a hydrazone substructure were designed and synthesized via a concise synthesis route. Bioassay results showed that most of the thiazole derivatives exhibited broad-spectrum fungistatic activities, which were exemplified by compounds 1c, 1e, 1g, 1h and 1j. In particular, compound 1e displayed excellent in vitro inhibitory effects with the EC₅₀ values of 5.00, 18.24, 6.94, and 3.03 μg/mL against the fungi Botrytis cinerea, Cytospora sp, Fusarium graminearum, and Fusarium solani, respectively. Detached fruit experiments against tomato gray mold (caused by B. cinerea) in vivo revealed that the control efficiency of compound 1e at 10, 20 and 40 μg/mL for 5 days was 35.05%, 54.14% and 81.83%, respectively, which was comparable and even superior to that of the fungicide carbendazim. Additionally, the title compounds also showed remarkable larvicidal activity against M. separata and some compounds exhibited good aphicidal activity. In a word, the bioassay indicated that a certain number of title compounds had multiple biological activities. Given their excellent antifungal and larvicidal characteristics, these interesting derivatives based on the title compounds could be served as new scaffolds for the development of pesticide with multifunctional applications.

Foodborne contaminants such as biogenic amines (BAs), nitrite and sulfite are harmful to human health. To safeguard food safety, the content of BAs, nitrite and sulfite should be strictly controlled. Small-molecule fluorescent probes are a promising analytical tool for monitoring BAs, nitrite and sulfite because they are highly sensitive and selective, offer simplicity of operation, and can enable optical signal visualization of the analyte. In this review, we summarize the most recent progress on the development of fluorescent probes for selectively detecting BAs, nitrite, and sulfite. In particular, we discuss the working mechanisms, sensing performance, and practical applications of various fluorescent probes that have been developed in recent years for detecting BAs, nitrite, and sulfite, with a particular emphasis on the utilization of these probes in food. Lastly, we discuss the research directions, trends, and prospects of molecular fluorescent probes in food applications in the future. We hope this review can offer conceptual and design guidance for researchers and practitioners to develop novel fluorescent probes for food safety.

To explore non-food bioactive products for pesticide candidates, and high value-added application of crop plants in agriculture, by using osthole (a natural coumarin isolated from a Chinese herbal medicine Cnidium monnieri) as a lead compound, a series of osthole derivatives containing oximoether groups were synthesized, and evaluated for their agricultural activities against Tetranychus cinnabarinus and Mythimna separata. The key steric configurations of eight derivatives were confirmed by X-ray crystallography. Especially compound 4r showed potential insecticidal activity (>2-fold of osthole) against M. separata, and 4g displayed good acaricidal activity against T. cinnabarinus (LC₅₀ = 0.566 mg/mL, > 2-fold of osthole). Their structure–activity relationships were also concluded. It will pave the way for future application of osthole derivatives as coumarin-kind botanical pesticides in crop protection.

Nicotine and nornicotine-typed compounds are well-known for its potential as insecticide. Some researches have shown that nicotine was highly toxic to Diaphorina citri Kuwayama, an invasive and fast spreading pest. Here we report the effects of nornicotine-typed insecticide against D. citri. Novel compounds A1-A8, B1–B28, C1–C18 and D1-D12 were synthesized by reported procedure. And bioassays indicated that some of these compounds exhibited good effects against D. citri. Compounds B2, B3, B8, B12, B13, B22, C5, C7, D5, and D9 exhibited the mortality up to 100% within 120 h in 50 mg/L. And further data shows that A2-5, A7, B1, B8, B20 and B22 showed rapid insecticidal activities against D. citri in 24 h with the low LC₅₀ (LC₅₀ < 50 mg/L in 24 h, and LC₅₀ < 30 mg/L in 72 h). Nornicotine-typed derivatives exhibited activity against D. citri, and B8 and B22 exhibited the best insecticidal activity with an LC₅₀ of 18.0 ± 1.0, 18.2 ± 0.9 mg/L in 24 h, which had the lower cost than nicotine and showed the potential as powerful insecticides.

Benzoxaborole, a five-membered oxaborole ring fused with a phenyl ring, has demonstrated potent pharmacological activity. In order to explore their potential applications in agriculture, five-membered and six-membered benzoxaborole derivatives were synthesized and evaluated for their fungicidal activity against six common plant pathogenic fungi in vitro. The bioassay results showed that most of the target compounds exhibited significant fungicidal activity at concentrations below 50 μg/mL, particularly the highlighted compounds 4b and 4e, which demonstrated impressive fungicidal activity superior to those of the positive controls. Molecular docking was also performed to confirm the practical value of the active compound as a potential inhibitor of Leucyl-tRNA Synthetase (LeuRS). This study indicates that the designed benzoxaborole derivatives could serve as template molecules for the development of novel fungicides.

We intended to highlight the interesting findings that three leucine-rich repeat receptor kinases function as receptors for sulfated plant peptide hormones, which could mediate switching between plant growth and stress tolerance. Thereafter, we proposed the potential of developing chemical regulators for promoting plant growth when they are suffering from environmental stresses.

The survival of human beings is inseparable from the development of agriculture. The use of pesticides is still an important means to ensure agricultural production, economic benefits and the national economy. With the abuse of pesticides, some pesticides are difficult to degrade after entering the natural world, which leads to many serious problems through the transmission and enrichment of food chains. Pesticide residue detection is a long-term challenge in the field of environment and food safety detection. In recent years, a large number of studies have been carried out on the detection of pesticide residues based on fluorescence sensing methods. This paper focuses on the application of fluorescence sensors in environmental samples or food, and analyzes the advantages and problems of existing fluorescence sensors in design, construction and data processing. Finally, the possible improvement directions in the future are discussed to promote its potential commercial value application research.

Graphite-derived carbon-based nanomaterials (GCNMs) as an exciting class of engineering carbonmaterials have been extensively exploited in environment and agriculture for pollution restorer, environmental purifier, plant growth stimulant, and stress resistance inducer. With the increasing demand of production in past decades, GCNMs were inevitably released into the natural environment and became emerging pollutants.

This review briefly summarized the recent progress on GCNMs-plant interaction with positive and negative sides, and discussed the biphasic (stimulatory-inhibitory) regulation of GCNMs on plant systems. The emphasis was placed on disseminating the latest scientific research, covering various effectiveness of GCNMs on plants and cells as well as nanotoxicity. Particularly, it is highlighted that fullerenes, carbon nanotubes, graphenes, and their functionalized forms as the representative zero-, one-, and two-dimensional GCNMs in optimum quantity have favorable efficacy on plants for seed germination, growth and development, fruit and productivity, and stress tolerance. On the contrary, GCNMs have possibly induced cytotoxicity and phytotoxicity on plant at anatomic, physiological, and genetic levels. The toxic mechanisms were mainly attributed to ion leakage from membrane, chloroplast damage, decreasing the levels of photosynthetic/nonphotosynthetic pigments and plant hormones, downregulating activities of metabolism and enzymatic/non-enzymatic antioxidant systems, or triggering ROS increase for inducing oxidative stress. This comprehensive review provides an in-depth insight of advanced progress made toward the utilization of GCNMs in plant science fields as well as current challenges. Future perspectives on a directional guide for further research in the emerging area of GCNMs-enabled phytonanotechnology are summarized at the end. This will possibly provide an important reference role for further study and rational application of GCNMs in agriculture.

As important physiological regulators, peptides have been used in many fields including medicine, cosmetics, healthcare products, animal nutrition and health, and plant nutrition and protection. In recent years, peptides have become a popular research subject in plant protection as antimicrobial and immune inducers, plant growth regulators, insecticides, and herbicides for their extensive raw material sources, excellent activity, and ideal environmental compatibility. This paper briefly introduces peptide research progress, presents an overview of peptide studies in plant protection, and summarizes the application of the peptides in plant protection and prospects for peptides as green agrochemicals.