5-(4-羟基苯基)-2,4-咪唑啉二酮酯类化合物的合成及其生物活性  

Synthesis and Biological Activities of 5-(4-Hydroxyphenyl)-2,4-imidazolidinedione Esters

作　　者：韩金涛[1] 王进敏[1] 陈守聪[1] 邱立红[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》2010年第5期691-697,共7页Chinese Journal of Organic Chemistry

基　　金：国家自然科学基金(No20772150);十一五科技支撑计划(No2006BAE01A01)资助项目

摘　　要：在模拟AdSS酶天然抑制剂结构合成5-(4-羟基苄基)-2,4-咪唑啉二酮酯系列化合物的基础上,为优化其结构,以5-(4-羟基苯基)-2,4-咪唑啉二酮为中间体,合成了28个未见文献报道的5-(4-羟基苯基)-2,4-咪唑啉二酮羧酸酯类化合物,它们的结构均经IR,1HNMR和元素分析表征.初步生物活性测试表明目标化合物5-(4-羟基苯基)-2,4-咪唑啉二酮对叔丁基苯甲酸酯(2i)和2-噻吩酸酯(3b)在浓度200μg/mL时对拟南芥生长抑制率达70%..Based on the 5-（4-hydroxybenzyl）-2,4-imidazolidinedione esters synthesized by simulating the structure of natural inhibitor of AdSS synthetase, twenty eight novel compounds 5-（4-hydroxyphenyl）-2,4- imidazolidinedione esters were synthesized using 5-（4-hydroxyphenyl）-2,4-imidazolidinedione as the key intermediate. Their structures were confirmed by m.p., IR, 1H NMR techniques and elemental analysis. The preliminary bioassay results indicated that 5-（4-hydroxyphenyl）-2,4-imidazolidinedione p-tert-butylbenzoate （2i） and 2-thiophenate （3b） have an inhibitory ratio 70% against Arabidopsis thaliana at the concentration of 200 μg/mL.

关 键 词：AdSS酶抑NN 5-(4-羟基苯基)-2 4-咪唑啉二酮羧酸酯 生物活性 

分 类 号：TQ252.3[化学工程—有机化工]