腺苷酸琥珀酸合成酶双基抑制剂类似物的合成及生物活性  

Synthesis and Herbicidal Activity of Adenylosuccinate Aynthetase Bisubstrate Hybrid Inhibitor Analogues

作　　者：刘斌[1] 孔令青[1] 董宏波[1] 王明安[1] 

机构地区：[1]中国农业大学应用化学系,北京100193

出　　处：《有机化学》2015年第12期2642-2649,共8页Chinese Journal of Organic Chemistry

基　　金：国家自然科学基金(No.20772150);国家十二五科技支撑计划(No.2011BAE06B04)资助项目~~

摘　　要：以丁内酯为原料,通过缩合、水解、亚胺化、关环、还原、偶联、甲酰化以及脱保护等反应设计并探索了腺苷酸琥珀酸合成酶双基抑制剂类似物的合成方法,目标化合物的结构经1H NMR和HR-ESI-MS数据进行表征.初步生物活性测试结果表明,目标化合物在100μg/m L浓度下对油菜和稗草具有较弱的抑制活性.The adenylosuccinate synthetase （AdSS） bisubstrate hybrid inhibitor analogues 5-（4-hydroxybenzyl）-N3- [5-ethoxyearbonyl-4-（N-formylhydroxyamino）pentyl]-hydantoin benzoates containing the structural moiety of hadacidin were designed and synthesized via Claisen condensation, hydrolysis decarbosylation, imidization, acid-catalyzed ring closure, borane reduction, Mitsunobu coupling reaction, formylation and deprotection used 1,4-butyrolactone as raw materials. Their structures were characterized with IH NMR and HR-ESI-MS data. The preliminary and greenhouse test results showed that these compounds only exhibited weak inhibition against E. rusgalli and B. campestris at the concentration of 100 lag/mL.

关 键 词：腺苷酸琥珀酸合成酶 双基抑制剂 Hadacidin 合成 除草活性 

分 类 号：O621.3[理学—有机化学]