Synthesis and Antifungal Activities of Novel Strobilurin Derivatives Containing Quinolin-2（1H）-one Moiety  

作　　者：LIU Ming LIU Yang ZHOU Sha ZHANG Xiao YU Shujing LI Zhengming 

机构地区：[1]State Key Laboratory of Elemento-organic Chemistry, Collaborative Innovation Center of Chemical Science and Engineering(Tianjin), Nankai University, Tianjin 300071, P. R. China

出　　处：《Chemical Research in Chinese Universities》2016年第4期600-606,共7页高等学校化学研究（英文版）

摘　　要：To discover novel lead compounds with better antifungal activities, a series of novel strobilurin derivatives containing quinolin-2（1H）-one moiety was designed and synthesized via intermediate derivatization method. Their structures were characterized by means of 1H nuclear magnetic resonance（IH NMR）, 13C NMR and high reso- lution mass spectrometry（HRMS）. The biological assay results indicate that most target compounds exhibit good to excellent fungicidal activities against 10 plant pathogens. Compounds 4d, 5b and 5c possess 94.1%, 83.8% and 80.9% in vitro inhibition respectively against Rhizotonia cereals at the concentration of 50 μg/mL, which are better than that of the control agents. Especially, the inhibition activities of compound 4d against all of the tested fungi approach or exceed those of the controls. The structure-activity relationship was also discussed.To discover novel lead compounds with better antifungal activities, a series of novel strobilurin derivatives containing quinolin-2（1H）-one moiety was designed and synthesized via intermediate derivatization method. Their structures were characterized by means of 1H nuclear magnetic resonance（IH NMR）, 13C NMR and high reso- lution mass spectrometry（HRMS）. The biological assay results indicate that most target compounds exhibit good to excellent fungicidal activities against 10 plant pathogens. Compounds 4d, 5b and 5c possess 94.1%, 83.8% and 80.9% in vitro inhibition respectively against Rhizotonia cereals at the concentration of 50 μg/mL, which are better than that of the control agents. Especially, the inhibition activities of compound 4d against all of the tested fungi approach or exceed those of the controls. The structure-activity relationship was also discussed.

关 键 词：STROBILURIN Fungicidal activity QUINOLINONE Intermediate derivatization method 

分 类 号：TQ455.4[化学工程—农药化工] TQ463.53