3位苯甲酰腙和亚氨基取代硫脲取代的吲哚满二酮衍生物的合成及对AHAS的抑制活性  

Design,Synthesis of 3-Substituted Benzoyl Hydrazone and 3-(Substituted Thiourea)yl Isatin Derivatives and Their Inhibitory Ativities of AHAS

作　　者：李慧东[1] 商建丽[1] 谭海忠[1] 王建国[1] 李永红[1] 李正名[1] 

机构地区：[1]南开大学元素有机化学研究所元素有机化学国家重点实验室,天津300071

出　　处：《高等学校化学学报》2010年第5期953-956,共4页Chemical Journal of Chinese Universities

基　　金：国家"九七三"计划项目(批准号:2010CB126103);国家自然科学青年基金(批准号:20602021);国家基金委中澳合作特别项目(批准号:20911120022)资助

摘　　要：基于前期生物设计AHAS抑制剂的研究,设计合成了15个吲哚满二酮类衍生物,其中9个为新化合物,其结构均经过1H NMR,MS和元素分析确证,并对所有化合物进行了离体和活体活性测试.实验结果表明,这类化合物在体内和体外均具有一定的生物活性,在离体活性测试中,所有化合物在100μg/mL浓度下对拟南芥AHAS均表现出明确的抑制活性,其中化合物4d,4e,5a和5f在10μg/mL浓度下仍然对AHAS表现出45%以上的抑制率,但此类化合物除草活性普遍较差.Based on the results of our previous bio-rational design of AHAS inhibitors research,15 isatin derivatives were designed and synthesized,anong which 9 compounds are new.Their structures were confirmed via 1H NMR,MS and elemental analysis.Preliminary bioassay showed that most of the isatin derivatives exhibited some inhibition aginast AHAS in vivo and in vitro.All the compounds exhibited good inhibition of Arabidopsis thaliana AHAS at the concentration of 100 μg/mL.Compounds 4d,4e,5a and 5f showed over 45% inhibition even at 10 μg/mL concentration.However,most compounds are week inhibitors in vivo,which means that other factors such as hydrophobicity should be considered in the future to enhance the in vivo activity.

关 键 词：AHAS抑制剂 吲哚满二酮类化合物 生物活性 

分 类 号：O626[理学—有机化学]