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

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.