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为了发现具有杀菌活性的新型先导化合物,基于几丁质合成酶催化作用机制,通过活性亚结构拼接方法,保留多氧霉素和尼克霉素中的活性尿苷部分,将具有良好杀菌活性的硫脲基团引入,设计合成了一系列含硫脲结构的核苷类化合物.以尿苷为原料,经5步反应制得目标物,其结构经IR,1H NMR及元素分析确证.初步生测结果表明,部分化合物对芦笋茎枯病(Phomopsisasparagi bubak)表现出明显的抑制活性,其中6m的抑制率在50μg/mL浓度下为97.2%,与相同浓度的多氧霉素B活性(100%)接近.
In order to find a novel lead compound with bactericidal activity, based on the catalytic mechanism of chitin synthase, active substructural splicing method was used to preserve the active uridine moiety in polyoxin and niacin, and the sulfur with good bactericidal activity Urea group, a series of nucleoside compounds with thiourea structures were designed and synthesized.Uridine was used as the starting material to make the target compound through 5 steps, and its structure was confirmed by IR, 1H NMR and elemental analysis. The results showed that some of the compounds showed obvious inhibitory activity against Phomopsis asparagi bubak. The inhibitory rate of 6m was 97.2% at the concentration of 50μg / mL, which was the same as that of the same concentration of polyoxin B (100%). Close to