Fu Ying, Wang Kui, Wang Peng, Kang Jing-Xin, Gao Shuang, Zhao Li-Xia, Ye Fei
Department of Applied Chemistry, College of Science, Northeast Agricultural University, Harbin, China.
Front Chem. 2019 Jan 22;7:2. doi: 10.3389/fchem.2019.00002. eCollection 2019.
4-Hydroxyphenylpyruvate dioxygenase (HPPD) is one of the most vital targets for herbicides discovery. In search for HPPD inhibitors with novel scaffolds, a series of aryl-naphthyl methanone derivatives have been designed and synthesized through alkylation and Friedel-Crafts acylation reactions. The bioassay indicated some of these compounds displayed preferable herbicidal activity at the rate of 0.75 mmol/m by post-emergence application, in which compound displayed the best herbicidal activity. The molecular docking showed that compound could bind well to the active site of the HPPD. This study shows that aryl-naphthyl methanone derivatives could be a potential lead structure for further development of novel herbicides.
4-羟基苯丙酮酸双加氧酶（HPPD）是除草剂研发中最重要的靶点之一。为了寻找具有新型骨架的HPPD抑制剂，通过烷基化和傅克酰基化反应设计并合成了一系列芳基萘基甲酮衍生物。生物活性测定表明，其中一些化合物在苗后施用时，以0.75 mmol/m的剂量表现出较好的除草活性，其中化合物表现出最佳的除草活性。分子对接表明，化合物可以很好地结合到HPPD的活性位点。该研究表明，芳基萘基甲酮衍生物可能是进一步开发新型除草剂的潜在先导结构。
