新型含嘧啶环的半乳糖苷类衍生物的合成及杀菌活性  

Synthesis and antimicrobial activities of novel galactoside derivatives containing a pyrimidine moiety

作　　者：陈美航 鲁道旺 张迅 杜士杰 李娜 马关康 吴文能 罗海荣 CHEN Meihang;LU Daowang;ZHANG Xun;DU Shijie;LI Na;MA Guankang;WU Wenneng;LUO Hairong(College of Material and Chemistry Engineering,Tongren University,Tongren 554300,Guizhou Province,China;College of Food and Phphmaceutical Engineering,Guiyang University,Guiyang 550005,China)

机构地区：[1]铜仁学院材料与化学工程学院,贵州铜仁554300 [2]贵阳学院食品与制药工程学院,贵阳550005

出　　处：《农药学学报》2021年第5期1024-1030,共7页Chinese Journal of Pesticide Science

基　　金：国家自然科学基金项目(21762037);贵州省科技计划项目(黔科合基础[2019]1454);绿色农药与农业生物工程教育部重点实验室(贵州大学)开放基金项目(黔教合KY字[2019]038);贵州省科技支撑计划项目黔科合支撑([2020]4Y097).

摘　　要：为寻找具有更高杀菌活性的含氮杂环化合物,合成了13个未见文献报道的新型含嘧啶环的半乳糖苷类衍生物,其结构经过核磁共振氢谱(^(1)H NMR)、碳谱(^(13)C NMR)和高分辨质谱(HRMS)等方法确证。杀菌活性测试结果表明:该类化合物对马铃薯晚疫病菌Phytophthora infestans、小麦赤霉病菌Gibberella zeae、水稻纹枯病菌Thanatephorus cucumeris、葡萄座腔病菌Botryosphaeria dothidea和拟茎点霉菌Phompsis sp.均具有较好的杀菌活性,其中化合物4m对马铃薯晚疫病菌的EC_(50)值分别为8.67μg/mL,与对照药剂烯酰吗啉(EC_(50)值8.34μg/mL)活性相当。此外,该类化合物对柑橘溃疡病菌Xanthomonas citri subsp.citri和水稻白叶枯病菌Xanthomonas oryzae pv.oryzae也有一定的杀菌活性。To find nitrogen heterocyclic derivatives with higher antimicrobial activities,thirteen novel galactoside derivatives containing a pyrimidine moiety were synthesized,and their structures were confirmed by ^(1)H NMR,^(13)C NMR and HRMS.The result of biological activity indicated that the target compounds possessed good antifungal activities against Phytophthora infestans,Gibberella zeae,Thanatephorus cucumeris,Botryosphaeria dothidea and Phompsis sp..Among them,compound 4m showed excellent antifungal activities against P.infestans,with the EC_(50) value of 8.67μg/mL,which were similar with that of dimethomorph(EC_(50) value 8.34μg/mL).Moreover,the target compounds exhibited certain antibacterial activities against Xanthomonas citri subsp.citri and Xanthomonas oryzae pv.oryzae.

关 键 词：嘧啶 半乳糖苷衍生物 合成 植物病原真菌 植物病原细菌 杀菌活性 

分 类 号：O626.417[理学—有机化学] S482.2[理学—化学]