Use of a quinazoline-diarylether derivative for inhibiting and / or controlling pathogenic microorganisms
By synthesizing quinazoline-diaryl ether derivatives, the problems of high toxicity and easy development of resistance in existing pesticides have been solved, achieving highly efficient inhibition and sterilization of plant pathogens. A new type of agricultural drug with low toxicity and environmental friendliness has been developed, which is suitable for the prevention and control of plant diseases such as rice bacterial blight and citrus canker.
Patent Information
- Authority / Receiving Office
- CN · China
- Patent Type
- Applications(China)
- Current Assignee / Owner
- GAUNGXI TIANYUAN BIOCHEM
- Filing Date
- 2026-03-25
- Publication Date
- 2026-06-09
AI Technical Summary
Existing chemical pesticides have problems such as high toxicity, easy development of resistance, and environmental pollution in the control of plant pathogens. There is a lack of research on combining quinazoline compounds and diaryl ether compounds, making it difficult to develop new pesticides that are novel in structure, highly efficient, low in toxicity, and environmentally friendly.
The design and synthesis of quinazoline-diaryl ether derivatives, which combine quinazoline and diaryl ether structures through specific chemical methods, have led to the development of novel drugs with inhibitory and bactericidal effects against plant pathogens such as rice bacterial blight pathogen and citrus canker pathogen. The specific synthesis method includes preparing diaryl ether intermediates using phenols with different substitutions and p-fluorobenzonitrile as raw materials, and constructing quinazoline-diaryl ether derivatives with 4-chloroquinazoline with different substitutions.
Quinazoline-diaryl ether derivatives exhibit excellent inhibitory and bactericidal activities against plant pathogens. Some compounds show significant inhibitory effects on rice bacterial blight and citrus canker, and have toxic and bactericidal activities against fungi such as Sclerotinia sclerotiorum, Botrytis cinerea, and southern root-knot nematodes. Moreover, they are easy to prepare and the raw materials are inexpensive and readily available, making them promising candidates for development into novel agricultural agents.
Smart Images
Figure CN122167363A_ABST
Abstract
Claims
1. The use of a quinazoline-diaryl ether derivative in inhibiting and / or preventing pathogenic microorganisms, characterized in that: The general structural formula of the quinazoline-diaryl ether derivative is: ； Among them, R in the general structural formula 1 It is one of the following: hydrogen-substituted, fluorine-substituted, chlorine-substituted, bromine-substituted, amino, nitro, and dimethoxy. R 2 It is one or two of the following: hydrogen substitution, fluorine substitution, tert-butyl substitution, methyl-tert-butyl substitution, trifluoromethoxy substitution, trifluoromethyl substitution, amino substitution, and fluorine-amino substitution.
2. The use according to claim 1, characterized in that, The structure of the quinazoline-diaryl ether derivative is selected from: 。 3. The use according to claim 1, characterized in that, The structure of the quinazoline-diaryl ether derivative is as follows: 。 4. The use according to claim 1, characterized in that, The synthesis of the quinazoline-diaryl ether derivatives with structures KZL-Z1 to KZL-Z20 is carried out according to the following reaction formula: 。 5. The use according to claim 1, characterized in that, The pathogenic microorganisms include agricultural pathogenic fungi, agricultural pathogenic bacteria, and agricultural pathogenic nematodes.
6. The use according to claim 5, characterized in that, The agricultural pathogenic fungi include Rhizoctonia solani. Rhizoctonia solani Sclerotinia sclerotiorum, Botrytis cinerea Botrytis cinerea Fusarium graminearum Fusarium graminearum Rice blast fungus Magnaporthe oryzae Fusarium pseudograss Fusarium pseudograminearum ; The agricultural pathogens include the pathogen causing rice bacterial blight. Xanthomonas oryzae ACCC 11602, Pathogen of Citrus Canker Xanthomonas axonopodis pv. Citri bacterial wilt pathogen Pseudo-monas sollamacearum ; The agricultural pathogenic nematodes include the southern root-knot nematode. Meloidogyne incongnita .
7. A pharmaceutical preparation for inhibiting and / or preventing pathogenic microorganisms, characterized in that, The pharmaceutical preparation includes the quinazoline-diaryl ether derivatives described above.
8. The pharmaceutical preparation according to claim 7, characterized in that, The quinazoline-diaryl ether derivative is the active ingredient in the pharmaceutical preparation, and its weight percentage is 1-99%.
9. The pharmaceutical preparation according to claim 7, characterized in that, The pharmaceutical preparation further includes pharmaceutically acceptable adjuvants selected from one or more of the following: dispersants, wetting agents, wetting and dispersing agents, fillers, emulsifiers, thickeners, dispersion media, disintegrants, solvents, preservatives, antifreeze agents, binders, specific gravity regulators, defoamers, oil-phase wall materials, aqueous-phase wall materials, and water.
10. The pharmaceutical preparation according to claim 7, characterized in that, The dosage form of the pharmaceutical preparation is one of the following: granules, dry suspension, aqueous suspension, dispersible oil suspension, microcapsule suspension, wettable powder, emulsifiable concentrate, water emulsion, water-dispersible granules, and seed treatment agent.