含取代苯甲酰基硫脲的核苷类化合物的合成及杀菌活性研究  

Synthesis and Fungicidal Activities of Nucleoside Compounds Containing Substituted Benzoyl Thiourea

作　　者：苗宏健[1] 张继伟[1] 袁会珠[2] 李映[1] 徐焱[1] 李慧[1] 杨新玲[1] 凌云[1] 

机构地区：[1]中国农业大学理学院应用化学系、农业部农药化学及应用重点开放实验室,北京100193 [2]中国农业科学院植物保护研究所,北京100193

出　　处：《有机化学》2012年第5期915-921,共7页Chinese Journal of Organic Chemistry

基　　金：国家自然科学基金(No.21072222);国家973计划(No.2010CB126104);‘十二五’科技支撑计划(No.2011BAE06B05-5)资助项目~~

摘　　要：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.To find new fungicidal lead compounds, based on the catalytic mechanism of chitin synthase, a series of novel nucleoside compounds containing thiourea were designed via the method of linking active sub-structures, in which the thio- urea with high fungicidal activity was combined to the uridine part ofpolyoxins and nikkomycins. The target compounds were synthesized from uridine in 5 steps. Their structures were confirmed by IR, 1H NMR spectra and elemental analysis. The pre- liminary bioassay results indicated that some compounds showed obvious inhibition effects against Phomopsisasparagi bubak, especially, and the fungicidal activity of 6m （97.2%） at 50 μg/mL is similar to that （100%） ofpolyoxin B.

关 键 词：几丁质 多氧霉素 尿苷 硫脲 杀菌活性 

分 类 号：O621.3[理学—有机化学]