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为了寻找高效广谱的植物激活剂候选化合物,以三乙胺为缚酸剂,通过4-甲基-1,2,3-噻二唑-5-甲酰氯与酚类化合物在二氯甲烷中于室温下反应,制得一系列共20个4-甲基-1,2,3-噻二唑-5-甲酸芳酯化合物,其中9个化合物未见文献报道,所有化合物的结构均得到了核磁共振氢谱、红外光谱、高分辨质谱的表征和确认。选择化合物2g培养了单晶,利用X-射线单晶衍射确证了该类化合物的空间结构。杀菌活性测定结果表明:部分化合物在50μg/mL下具有显著的离体杀菌活性,其中化合物2c,2n和2o具有广谱的杀菌活性,其EC50值在3.46～23.30μg/mL之间。生物活性测定结果表明,部分化合物显示了较好的抗病毒活性,大部分化合物对烟草花叶病毒(TMV)具有较好的钝化效果,2a,2c,2d,2e,2f,2g,2l,2o具有较好的诱导烟草抗TMV的活性。
In order to find efficient broad-spectrum plant activator candidate compounds, triethylamine as an acid-binding agent, 4-methyl-1,2,3-thiadiazole-5-carboxylic acid chloride and a phenolic compound in methylene chloride At room temperature, a series of 20 aryl compounds of 4-methyl-1,2,3-thiadiazole-5-carboxylic acid were obtained, of which 9 compounds were not reported and the structures of all compounds were obtained Characterization and confirmation of proton nuclear magnetic resonance, infrared spectroscopy and high resolution mass spectrometry. The compound 2g was cultured in single crystal and the spatial structure of the compound was confirmed by X-ray single crystal diffraction. The results of the bactericidal activity test showed that some compounds exhibited significant in vitro bactericidal activity at 50 μg / mL. Among them, compounds 2c, 2n and 2o exhibited a broad range of bactericidal activity with EC50 values between 3.46 and 23.30 μg / mL. The bioassay results showed that some of the compounds showed good antiviral activity and most of the compounds had good passivation effect against tobacco mosaic virus (TMV). 2a, 2c, 2d, 2e, 2f, 2g, 2l, 2o has a better induction of tobacco anti-TMV activity.