一些吲哚二酮类衍生物的合成及对AHAS的抑制活性

Synthesis of Isatin Derivatives and Their Inhibition Against AHAS

基于一些新结构特征的AHAS抑制剂,设计并合成了一系列吲哚二酮类化合物.初步的生物活性测试结果表明,所合成的化合物在体内和体外均具有一定的生物活性,其中,化合物13在100μg/mL浓度下对AHAS的抑制达到85%,化合物7(平皿法)在100μg/mL浓度条件下对油菜胚根生长抑制率可达84.7%,是一类未见文献报道的结构新型的AHAS抑制剂,有望为进一步设计合成更高活性的化合物提供参考.

Based on the crystal structure of AHAS enzyme, bio-rational drug design was used to discover some novel AHAS inhibitors via computational virtual screening. Some isatin derivatives as AHAS inhibitors were designed, synthesized and evaluated. The preliminary results show that the isatin compounds exhibit conside- rate inhibition both in vivo and in vitro against AHAS. Compound 13 show an inhibition of 85% at 100μg/mL concentration in vitro and compound 7 show an inhibition of 84.7% of rape root length at 100 μg/mL concen-tration. This discovery provides meaningful information for further design and synthesis of novel compounds with enhanced activity.