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3,4,6-Trisubstituted-alpha-pyrone derivative and preparation method and application thereof

A technology of pyrone and derivatives is applied in the application field of preparing tomato gray mold inhibitor, and can solve problems such as drugs that have not yet been seen

Active Publication Date: 2018-04-24
NINGBO UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

There is no report on the chemical structure of the compound and the activity against Botrytis cinerea, so there is no drug related to it on the market

Method used

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  • 3,4,6-Trisubstituted-alpha-pyrone derivative and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] A 3,4,6 trisubstituted-α-pyrone derivative structural formula is shown in I:

[0024] (I).

Embodiment 2

[0026] The preparation method of 3,4,6 three substituted-alpha-pyrone derivatives as shown in formula I, specifically comprises the following steps:

[0027] (1) Fermentation production

[0028] Aspergillus versicolor ( Aspergillus versicolor DJ013) was revived by streaking, transferred to a 250mL Erlenmeyer flask containing 100mL PDB medium, and cultured at 28°C and 180 r / min for 4 days to obtain a seed culture solution, and then the inoculum was inoculated with a volume ratio of 10%. The seed solution was inoculated into a 1000mL Erlenmeyer flask containing rice culture medium (prepared by dissolving 80g rice and 1g yeast powder in 120mL seawater), and cultured at 28°C for 35 days to obtain a fermented product;

[0029] (2) Obtaining the extract

[0030] Soak the above-mentioned fermented product in 4L of methanol for 3 times, then concentrate and evaporate the methanol extract to dryness, redissolve it in 1L of water, repeat the extraction 3 times with 1L of ethyl acetate...

Embodiment 3

[0038] In vitro anti-Botrytis cinerea test (96-well plate antibacterial method)

[0039] (1) Experimental samples

[0040] Preparation of the test sample solution: the test sample is the pure compound I isolated and purified in Example 1 above, and an appropriate amount of sample is accurately weighed, and prepared into a solution of the required concentration with DMSO for testing the activity.

[0041] (2) Experimental method

[0042] 96-well plate method: prepare 1 mg / mL DMSO sample solution of the compound to be tested, and in a 96-well plate, use sterilized PDB liquid medium to dilute to concentrations of 200, 100, 50, 25, 12.5, 6.25 μg / mL solution (50μL), add an equal amount of 1×10 6 CFU bacterial suspension, the final concentration is: 200, 100, 50, 25, 12.5, 6.25, 3.13μg / mL, shake well, and all the above operations are under sterile conditions. DMSO was used as blank control and carbendazim was used as positive control, and each treatment was repeated 3 times. The...

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Abstract

The invention discloses 3,4,6-trisubstituted-alpha-pyrone derivative and preparation and application thereof. The 3,4,6-trisubstituted-alpha-pyrone derivative is characterized in that a structural formula of the 3,4,6-trisubstituted-alpha-pyrone derivative is shown as in formula I, and a preparation method comprises the steps of subjecting Aspergillus versicolor with a preservation number of CCTCCNo. M2014089 to fermentation culture to obtain a fermented product containing novel 3,4,6-trisubstituted-alpha-pyrone derivative, soaking the fermented product in methanol, extracting with ethyl acetate to obtain crude extract, subjecting the crude extract to reduced pressure silica-gel column chromatography, performing reversed-phase semi-preparative high-performance liquid chromatography, separating, and purifying to obtain the 3,4,6-trisubstituted-alpha-pyrone derivative. The 3,4,6-trisubstituted-alpha-pyrone derivative can resist Botrytis cinerea and has the advantage that the derivativemay act as a novel pharmaceutical ingredient or lead compound for Botrytis cinerea inhibitors.

Description

technical field [0001] The present invention relates to a 3,4,6 trisubstituted-α-pyrone derivative, in particular to a method for preparing a 3,4,6 trisubstituted-α-pyrone derivative with marine Aspergillus and the Application of compounds in the preparation of inhibitors of Botrytis cinerea. Background technique [0002] Microorganisms have always been an important resource for the development of biopesticides. Microbial-derived biopesticides such as jinggongmycin, kasugamycin, polyoxin, agriculturalantibiotic 120, wuyiencin ( wuyiencin M), Qingfengmycin (qingfengmycin) and so on have been widely used in the control of plant diseases. But in recent years, the repeated discovery of the same chemically active substances has puzzled researchers in this field for a long time. Therefore, it has become a top priority and has very important social significance to continuously expand the screening objects, discover new agricultural antibacterial substances, and develop more agric...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D309/36C12P17/06A01N43/16A01P3/00C12R1/66
Inventor 肖烨丁立建何山姚佳晓孙晴镁
Owner NINGBO UNIV
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