百里香酚噁二唑衍生物的合成及生物活性研究  

Synthesis and biological activity of thyme thioether derivatives

作　　者：陈惠丽 张江 王治 韦兴菊 贺银菊 杨再波 CHEN Hui-li;ZHANG Jiang;WANG Zhi;WEI Xing-ju;HE Yin-ju;YANG Zai-bo(School of Chemistry and Chemical Engineering,Qiannan Normal University for Nationalities,Duyun 558000,China;Guizhou Provincial Academy of Higher Learning National Medicinal Plant Resources Development Engineering Research Center,Duyun 558000,China)

机构地区：[1]黔南民族师范学院化学化工学院,贵州都匀558000 [2]贵州省普通高等学校民族药用植物资源开发工程研究中心,贵州都匀558000

出　　处：《化学研究与应用》2018年第8期1224-1231,共8页Chemical Research and Application

基　　金：贵州省大学生创新创业训练计划重点项目(201610670009)资助;2014贵州省普通高等学校民族药用植物资源开发工程研究中心项目(黔教合KY字[2014]227号)资助;2017年度黔南民族师范学院化学一流学科专项资助计划项目(QNSYHX2017yl001)资助

摘　　要：以百里香酚为起始原料,经溴乙酸乙酯醚化后,再肼解后关环和硫醚化反应,共合成了16个未见报道的含噁二唑硫醚结构百里香酚衍生物。其结构经1HNMR、13CNMR表征和元素分析,并初步测定其抑制辣椒枯萎病菌(F.oxysporum)、苹果腐烂病菌(C.mandshurica)、半夏立枯病菌(R.solani)、油菜菌核病菌(S.sclerotiorum)的活性。结果表明,目标化合物对所有供试病菌均有一定的抑菌活性,其中,化合物4g、4h、4i、4j和4l对辣椒枯萎病菌、苹果腐烂病菌、半夏立枯病菌(R.solani)和油菜菌核病菌的抑制活性最好,均优于阳性对照百里香酚和唑菌酯。Using thymol as starting materials,sixteen novel thymol derivatives containingthioether structure were synthesized by etherification,hydrazine,cyclization and thioether.The structures of target compounds were fully characterized by 1H NMR,13 C NMR,and elemental analysis.and the activity to inhibit F.oxysporum,C.mandshurica,R.solani,and S.sclerotiorum were determined.The results showed that the target compounds showed antibacterial activity against all the tested bacteria.compounds 4g,4h,4i,4j and 4l had the best inhibitory activity against F.oxysporum,C.mandshurica,R.solani,and S.sclerotiorum,all of which were superior to those of positive control thyme and sulfisoxazole.

关 键 词：百里香酚 噁二唑硫醚 抗菌活性 合成 

分 类 号：O625.31[理学—有机化学]