- Design, Synthesis, Antiviral Bioactivity, and Defense Mechanisms of Novel Dithioacetal Derivatives Bearing a Strobilurin Moiety
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A series of dithioacetal derivatives bearing a strobilurin moiety were designed and synthesized on the basis of our previous work. The antiviral activities of these compounds against Potato virus Y (PVY), Cucumber mosaic virus (CMV), and Tobacco mosaic virus (TMV) were systematically evaluated. Bioassay results indicated that C14 elicited excellent curative and protective activities against PVY, CMV, and TMV. The former had 50% effective concentrations (EC50) of 125.3, 108.9, and 181.7 μg/mL, respectively, and the latter had 148.4, 113.2, and 214.6 μg/mL, respectively, which were significantly superior to those of lead compound 6f (297.6, 259.6, and 582.4 μg/mL and 281.5, 244.3, and 546.3 μg/mL, respectively), Ningnanmycin (440.5, 549.1, and 373.8 μg/mL and 425.3, 513.3, and 242.7 μg/mL, respectively), Chitosan oligosaccharide (553.4, 582.8, and 513.8 μg/mL and 547.3, 570.6, and 507.9 μg/mL, respectively), and Ribavirin (677.4, 690.3, and 686.5 μg/mL and 652.7, 665.4, and 653.4 μg/mL, respectively). Moreover, defensive enzyme activities and RT-qPCR analysis demonstrated that the antiviral activity was associated with the changes of SOD, CAT, and POD activities in tobacco, which was proved by the related proteins of abscisic acid signaling pathway. This work provided a basis for further design, structural modification, and development of dithioacetal derivatives as new antiviral agents.
- Chen, Jin,Shi, Jing,Yu, Lu,Liu, Dengyue,Gan, Xiuhai,Song, Baoan,Hu, Deyu
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- Synthesis and bio-evaluation of natural butenolides-acrylate conjugates
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A series of novel 3-aryl-4-hydroxy-2(5H) furanone-acrylate hybrids were designed and synthesized based on the natural butenolides and acrylates scaffolds. The structures of the prepared compounds were characterized by 1H-NMR, 13C-NMR and electrospray ionization mass spectrometry (ESI-MS), and the bioactivity of the target compounds against twelve phytopathogenic fungi was investigated. The preliminary in vitro antifungal activity screening showed that most of the target compounds had moderate inhibition on various pathogenic fungi at the concentration of 100 mg·L?1, and presented broad-spectrum antifungal activities. Further studies also indicated that compounds 7e and 7k still showed some inhibitory activity against Pestallozzia theae, Sclerotinia sclerotiorum and Gibberella zeae on rape plants at lower concentrations, which could be optimized as a secondary lead for further research.
- Bao, Longzhu,Wang, Shuangshuang,Song, Di,Wang, Jingjing,Cao, Xiufang,Ke, Shaoyong
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- A 2 - bromo methyl of compounds of preparation method
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The invention discloses a method for preparing a 2-benzyl bromide compound. The method comprises the following steps: carrying out a contact reaction on a compound shown as a formula (2), an organic solvent and bromate in the presence of hydrosulphite and a catalyst, thereby obtaining a compound shown as a formula (1), wherein the structural formula is as shown in the description, and in the formula (1) and the formula (2), R1 refers to C1-C4 alkyl, R2 refers to C1-C4 alkyl, X refers to nitrogen atoms or oxygen atoms, and Z refers to CH or nitrogen atoms. According to the method for preparing the 2-benzyl bromide compound disclosed by the invention, the operation conditions are simple, the bromine utilization rate is high, corrosive gases are avoided, harm to the environment is avoided, the target product is high in selectivity and high in yield, and the method is mild in production conditions and low in production cost. Therefore, the method can be suitable for large-scale industrial production.
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Paragraph 0046; 0049; 0050
(2017/12/05)
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- A METHOXYL ACRYLIC ESTER FUNGICIDE, THE PREPARATION METHOD AND USES THEREOF
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A methoxyl acrylic ester fungicide, the preparation method and uses thereof. The fungicide contains at less the following compound of formula (I) as active ingredient. The fungicide can be further prepared to form the emulsifier oil by mixing with the emulsifier, latent solvent, stabilizer, and solvent. The fungicide is useful for preventing and controlling powdery mildew, downy mildew, gray mold and tan discase of vegetable, melon and fruit, discase of vegetable, melon and fruit cased by Phoma citricarpa, leaf spot of maize, false smut, blossom-end rot of orange and Sclerotinia rot of colza et al. The fungicide has many advantages such as be effect to the strain which produced the resistance, high effect, less toxic and environmrnt-friendly.
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- METHOXYACRYLATE-BASED FUNGICIDE AND METHODS FOR PREPARING AND USING THE SAME
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A pharmaceutical composition of fungicide including at least a compound represented by Formula (I). The pharmaceutical composition of fungicide can further include an emulsifier, a cosolvent, a stabilizer, and a solvent. The fungicide can prevent and treat powdery mildew, downy mildew, gray mold, brown spot, scab of vegetables and fruits, southern leaf blight of corn, rice false smut, citrus stem-end rot, and rape sclerotinia rot, with high efficiency, low toxicity, and relative environmental friendliness. A method of preparing the fungicide and a method of using thereof are also provided.
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Page/Page column 3
(2010/12/18)
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- Process for producing acrylic acid derivative
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Processes for producing a compound represented by the formula (1), which includes an acrylic acid derivative and is useful as an agricultural chemical or medicine. One of the processes comprises the step of formulating a compound (3) and converting the OH of the resultant compound (2) into OR″. The first step comprises reacting a formic or orthoformic ester in the presence of a Lewis acid and a base. The second step comprises reacting the compound with R″OH or with R″OH and CH(OR″)3 under acidic conditions or using a phase-transfer catalyst in a two-phase system and regulating the base and the concentration thereof to stereoselectively synthesize the target compound. In another, process, the compound is efficiently produced without isolating the compound. The compound can also be produced without the compound (2).
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