【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.更多还原

【Abstract】 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.更多还原