Application of voriconazole to preparation of bactericide for controlling phytopathogens

A technology of plant pathogenic bacteria and voriconazole, which is applied in the application field of voriconazole and fungicides, can solve problems such as harm, kill non-target organisms, and drug residues, and achieve the effects of environmental friendliness, broad market application prospects, and good inhibitory activity.

Inactive Publication Date: 2019-02-15
QINGDAO AGRI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The long-term use of large quantities of chemical pesticides not only leads to resistance problems, but also causes pesticide residues, kills non-target organisms, pollutes the ecological environment, and eventually causes harm to the human body through bioaccumulation

Method used

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  • Application of voriconazole to preparation of bactericide for controlling phytopathogens
  • Application of voriconazole to preparation of bactericide for controlling phytopathogens
  • Application of voriconazole to preparation of bactericide for controlling phytopathogens

Examples

Experimental program
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Effect test

Embodiment 1

[0026] The present invention screened and synthesized the small molecule compound voriconazole based on the three-dimensional structure design of the Fusarium graminearum CYP51B protein (sterol demethylation inhibitor target protein) in the InterBioScreen database (https: / / www.ibscreen.com / ).

[0027] Chemical name: (2R,3S)-2-(2,4-difluorophenyl)-3-(5-fluoro-4-pyrimidine)-1-(1H-1,2,4-triazole-1- base) -2-butanol;

[0028] English:

[0029] (2R,3S)-2-(2,4-difluorophenyl)-3-(5-fluoropyrimidin-4-yl)-1-(1H-1,2,4-triazol-1-yl)butan-2-ol ; (2R,3S)-2-(2,4-Difluorophenyl)-3-(5-fluoro-4-pyrimidinyl)-1-(1H-1,2,4-tria zol-1-yl)-2- butanol, molecular formula: C 16 h 14 f 3 N 5 O, molecular weight: 349.115, structural formula as follows:

[0030]

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Abstract

The invention discloses application of voriconazole to preparation of a bactericide for controlling phytopathogens. Measurement on indoor drug sensitivity proves that the voriconazole has high inhibitory activity on main diseases of important grain crops, including fusariumgraminearum and maize curvularia; moreover, the voriconazole has high inhibitory activity on macrophomakawatsukai causing apple ring rot, valsaceratosperma causing apple rot and alternariatenuissima causing leaf spot of fruits and vegetables; furthermore, the voriconazole has relatively high inhibitory activity on soil-bornediseases extremely difficultly controlled in agricultural production, such as fusariumoxysporum, and the bacteriostatic activity thereof is even higher than that of the conventional bactericides suchas carbendazim and tebuconazole. The problem of a poor control effect caused by resistance of the plant pathogenic fungi such as the fusariumgraminearum and the macrophomakawatsukai to the existing bactericides can be effectively solved; and the voriconazole is environment-friendly and pollution-free, meets residual drug toxicity standards of the World Health Organization, and has a broad marketapplication prospect.

Description

technical field [0001] The invention belongs to the technical field of plant protection, and in particular relates to the application of voriconazole in the preparation of fungicides for preventing and controlling plant pathogenic bacteria. Background technique [0002] The Food and Agriculture Organization of the United Nations (FAO) estimates that the loss of crop production in the world is about 40% (440-550 billion yuan) due to damage from diseases, insect pests and weeds, and the impact on trees is even more difficult to estimate. The losses recovered through the work of scientists and various technology extension personnel engaged in pest research all over the world reached 300-400 billion yuan. For a long time, chemical control has been the main means of controlling plant diseases. The long-term use of large quantities of chemical pesticides not only leads to resistance problems, but also causes pesticide residues, kills non-target organisms, pollutes the ecological ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A01N43/653A01P3/00
CPCA01N43/653
Inventor 黄金光孙慧琳赵彦翔孙晓梅张淑颖
Owner QINGDAO AGRI UNIV
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