【摘要】 在对乙酰乳酸合成酶(AHAS)抑制剂进行生物合理设计的基础上,分别以4-氟-3硝基苯胺和2-胺基-5硝基苯腈为原料,合成了8个苯磺酰胺基苯甲酰胺类化合物和7个双苯磺酰胺基苯甲酰胺类化合物,其结构通过核磁共振谱、质谱、红外光谱及元素分析验证.初步的生物活性测定结果表明,部分化合物在体内和体外均具有一定的生物活性,其中化合物4c,4d和7c在100μg/mL浓度下对拟南芥AHAS的抑制率分别为66%,76%和68%,而化合物4a,4c,7a和7b在100μg/mL浓度下对油菜根长的抑制率分别为76%,70%,89%和82%.研究结果为进一步设计合成潜在的AHAS抑制剂提供了有益参考.更多还原

【Abstract】 Based on the strategy of bio-rational design of AHAS inhibitors,8 novel N-(phenylsulfonamidophenyl)benzamide and 7 novel N-{[N-(phenylsulfonyl)phenylsulfonamido] phenyl}benzamide derivatives were designed and synthesized by starting materials 4-fluoro-3-nitroaniline and 2-amino-5-nitrobenzonitrile,and their structures were confirmed by IR,MS,1H NMR and elemental analysis.The preliminary bioassay indicated that some compounds exhibited bioactivity either in vitro or in vivo.Compounds 4c,4d and 7c show inhibition to Arabidopsis thaliana AHAS of 66%,76% and 68% at 100 μg/mL.Compound 4a,4c,7a and 7b show inhibition on the growth of rape root of 76%,70%,89% and 82% at 100 μg/mL.The present results provide helpful guidance to further design more potential AHAS inhibitors.更多还原