Application of 1,3,4-thiadiazole compounds to prevention and treatment of rice xanthomonas oryzae

A technology for rice bacterial blight and rice bacterial blight, which is applied in the fields of application, animal repellent, plant growth regulator, etc., to achieve the effect of inhibiting, expanding application prospects, and high yield

Active Publication Date: 2018-01-05
SOUTH CHINA AGRI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The 1,3,4-thiadiazole fungicides such as Dicumazole and Bis-ADTA used to be effective agents for the control of rice bacterial blight, a refractory disease of rice, but due to the serious teratogenic effect and the growing problem of drug resistance

Method used

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  • Application of 1,3,4-thiadiazole compounds to prevention and treatment of rice xanthomonas oryzae
  • Application of 1,3,4-thiadiazole compounds to prevention and treatment of rice xanthomonas oryzae
  • Application of 1,3,4-thiadiazole compounds to prevention and treatment of rice xanthomonas oryzae

Examples

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Embodiment 1

[0038] Example 1: S-1,3,4-thiadiazole-5-(4-chlorophenyl)-2-furan thiocarbamate (H-4) and S-(5-methyl-1, Preparation of 3,4-thiadiazole)-5-(4-chlorophenyl)-2-furyl thiocarbamate (H-23)

[0039]

[0040] Add 15mmol 1,3,4-thiadiazole-2-thiol (or 5-methyl-1,3,4-thiadiazole-2-thiol) and 10mL di Chloromethane was added at room temperature with a 10% (wt.) solution containing 15 mmol of sodium hydroxide, and the rate of addition was controlled to keep the temperature at room temperature. After this was completed, a dichloromethane solution containing 7.5 mmol of 5-(4-chlorophenyl)-2-furoyl chloride was added dropwise. Control the rate of addition so that both are added at the same time. After the dropwise addition, slowly raise the temperature to 50°C, and react at 50°C for 3-10 hours. After the reaction was completed, filter to remove the precipitate, and rotate the filtrate to remove the solvent to obtain a light yellow solid. Compound H-4 was separated with a silica gel colum...

Embodiment 2

[0045] Compound shown in embodiment 2 formula I is to rice bacterial blight T3SS inhibitory activity

[0046] Pathogenic bacteria tested: Xoo wild-type strain PXO99 A and the corresponding mutant strain (hpa1inPXO99 A ), mainly causing rice bacterial blight. Test compound concentration: 10 μg / mL. 1. Experimental operation: Screening of inhibitors of Xanthomonas oryzae type Ⅲ secretion system (T3SS)

[0047] High-throughput screening based on various reporter genes is currently a general method for screening T3SS inhibitors, and green fluorescent protein (GFP) reporter gene combined with flow cytometry is one of the commonly used screening systems. In this study, a GFP reporter gene screening system based on the hpa1 (harpin protein) promoter region in Xoo was used. The expression of hpa1 is induced by the T3SS induction medium XOM2 and regulated by hrpX. A total of 30 compounds were screened, and it was determined that 21 compounds had an inhibitory rate of more than 60% ...

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PUM

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Abstract

The invention discloses application of 1,3,4-thiadiazole compounds to prevention and treatment of rice xanthomonas oryzae. The structural general formula of the compounds is as shown in the formula I.The compounds with the general formula have remarkable inhibiting effects on the activity of an hpa1 promoter. Part of the compounds has a remarkable inhibiting effect on a key virulence factor T3SSunder the condition of not influencing the normal growth of the rice xanthomonas oryzae, so the 1,3,4-thiadiazole compounds can be applied to prevention and treatment of the rice xanthomonas oryzae well.

Description

technical field [0001] The invention belongs to the application field of heterocyclic compounds, in particular to the application of 1,3,4-thiadiazole compounds in preventing and treating rice bacterial blight. Background technique [0002] In recent years, with the in-depth research on heterocyclic compounds with good biological activity and novel structure, more and more researchers have devoted themselves to the design and synthesis of various heterocyclic compounds. Among them, there are more and more researches on 1,3,4-thiadiazoles, and many 1,3,4-thiadiazoles are commercialized and put into use in pesticides. [0003] (1) Agricultural fungicides [0004] The 1,3,4-thiadiazole fungicides such as Dicumazole and Bis-ADTA used to be effective agents for the control of rice bacterial blight, a refractory disease of rice, but due to the serious teratogenic effect and the growing problem of drug resistance. Later, it was reported that the compound obtained after introduci...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A01N43/824A01P1/00
Inventor 崔紫宁陶辉田浩向绪稳姜珊张炼辉
Owner SOUTH CHINA AGRI UNIV
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