A5086131167- Fungal Plant Pathogen Control
- Synthesis and Biological Evaluation
- Synthesis and biological activity
- Plant-Microbe Interactions and Immunity
- Plant Disease Resistance and Genetics
- Insect Resistance and Genetics
- Radical Photochemical Reactions
- Insect-Plant Interactions and Control
- Catalytic C–H Functionalization Methods
- Sulfur-Based Synthesis Techniques
- Fluorine in Organic Chemistry
Nankai University
2022-2025
Institute of Organic Chemistry
2025
Defluorinative alkylation and arylation between thianthrenium salts α-trifluoromethyl alkene to afford gem -difluoroolefins by easily recycling thianthrene under visible light irradiation free of metal photocatalyst.
Lead discovery and molecular target identification are important for developing novel pesticides. Scaffold hopping, an effective approach of modern medicinal agrochemical chemistry a rational design molecules, is aiming to molecules with similar structures similar/better biological performance. Herein, 24 new ferimzone derivatives were designed synthesized by scaffold-hopping strategy. In vitro bioassays indicated that compound 5o showed potency against Cercospora arachidicola 2-fold higher...
The main challenge in the development of agrochemicals is lack new leads and/or targets. It critical to discover molecular targets and their corresponding ligands.
The discovery of novel leads and new targets is an important approach to address the issue fungicide resistance by development. indole skeleton has been widely utilized in agrochemicals due its unique biological activity. YZK-C22 a potent pyruvate kinase inhibitor with high antifungal Several were developed based on YZK-C22. Inspired these, [1,2,4]triazino[4,5-a]indol-1(2H)-one derivatives designed using hopping strategy; however, these compounds exhibited moderate fungicidal Unexpectedly,...
Oxysterol binding protein (OSBP) is a new target for oomycide development. To find more fungicidal active compounds targeting OSBP, series of carboxamides containing spiropiperidinyl-α-methylene-γ-butyrolactone and heterocyclic carboxylic acids were rationally designed synthesized by using computer-aided pesticide design method. The in vitro bioassay found that compound 5o showed broad-spectrum activity with EC50 values falling between 0.50 20.85 μg/mL against Phytophthora capsici Fusarium...
In this study, we developed a photoredox-catalyzed defluorinative cross-coupling method for trifluoroketones and alkyl boronic acids. The reaction afforded series of novel α,α-difluoroketone derivatives, in vitro fungicidal activity revealed that some these compounds exhibited moderate to excellent against Rhizoctonia solani Botrytis cinerea. particular, compound 3d showed an EC50 value 4.27 μg/mL B. cinerea can be used as lead further optimization.
Target based molecular design via the aid of computation is one most efficient methods in discovery novel pesticides. Here, a combination comparative field analysis (CoMFA) and docking was applied for potent fungicidal [1,2,4]-triazolo-[3,4-b][1,3,4]-thiadiazoles. Bioassay results indicated that synthesized target compounds 3a, 3b, 3c exhibited good activity against Alternaria solani, Botrytis cinerea, Cercospora arachidicola, Fusarium graminearum, Physalospora piricola, Rhizoctonia...
1,2,3-Thiadiazoles are among the most important heterocyclic motifs, with wide applications in natural products and medicinal chemistry. Herein, we disclose a tandem reaction for synthesis of structurally diverse 1,2,3-thiadiazoles from 3,4-dichloroisothiazol-5-ketones hydrazines. This method is characterized by mild external oxidant- sulter-free conditions, broad substrate scope, easy purification.
The development of new fungicides is vital for safeguarding crops and ensuring sustainable agriculture. Building on our previous finding that 4-(3,4-dichloroisothiazole)-7-hydroxy coumarins can be used as fungicidal leads, 44 novel coumarin ester derivatives were designed synthesized to evaluate whether esterification could enhance their activity. In vitro bioassays indicated compound 2ai displayed good activity against Alternaria solani, Botrytis cinereal, Cercospora arachidicola,...