新型2-取代苯甲酰基-5-烷基环戊酮的设计、合成与生物活性研究
收稿日期: 2012-08-28
修回日期: 2012-09-22
网络出版日期: 2012-09-26
基金资助
国家973计划(No. 2010CB126103);国家自然科学基金(Nos. 20772066, 21072108)和“十二五”科技支撑计划(No. 2011BAE06B05-3)资助项目.
Design, Synthesis and Bioactivity of Novel 2-Aroyl-5-alkylcyclopentanone Derivatives
Received date: 2012-08-28
Revised date: 2012-09-22
Online published: 2012-09-26
Supported by
Project support by the National Basic Research Program of China (973 Program) (No. 2010CB126103), the National Natural Science Foundation of China (Nos. 20772066, 21072108) and the National Key Technologies R&D Program (No. 2011BAE06B05-3).
为了发现具有良好生物活性的新型先导化合物, 在综合多种高活性化合物结构特点的基础上, 设计合成了一系列含苯甲酰基乙烯醇结构的2-取代苯甲酰基-5-烷基-环戊酮类化合物. 以己二酸二乙酯为原料, 经6步反应制得目标产物, 其结构经IR, 1H NMR, X射线及元素分析或高分辨质谱确证, 并对该类化合物合成方法进行了探讨. 初步生测结果表明, 部分化合物对油菜表现出明显的抑制活性, 在100 μg/mL浓度下对油菜的抑制率达到60%以上.
关键词： 对羟基苯基丙酮酸双氧化酶; 芳酰基乙烯醇; 环戊酮; 除草活性
徐海珍 , 朱有全 , 谢丽芬 , 王晓芳 . 新型2-取代苯甲酰基-5-烷基环戊酮的设计、合成与生物活性研究[J]. 有机化学, 2013 , 33(01) : 143 -147 . DOI: 10.6023/cjoc201208029
To find new lead compounds with muti-bioactivities, a series of novel 2-aroyl-5-alkylcyclopentanone derivatives containing 2-bezoylenthenol were designed on the base of various commercial products. The target compounds were synthesized from diethyl adipate in 6 steps. Their structures were confirmed by IR, 1H NMR spectra, X-ray and elemental analysis or HRMS. The preliminary bioassay results indicated that some compounds showed obvious inhibition effects against Brassica campestris, and the herbicidal activities were more than 60% at 100 μg/mL.
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