Design, Synthesis and Fungicidal Activity against Rhizoctonia solani of New Phenylpyrazoloxyl Propionic Acid Derivatives

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	Design, Synthesis and Fungicidal Activity against Rhizoctonia solani of New Phenylpyrazoloxyl Propionic Acid Derivatives
其他题名	Design, Synthesis and Fungicidal Activity against Rhizoctonia solani of New Phenylpyrazoloxyl Propionic Acid Derivatives
	Yu Fuqiang; Guan Aiying; Sun Xufeng; Li Huichao; Li Xiaowu
	2019
发表期刊	CHINESE JOURNAL OF ORGANIC CHEMISTRY
ISSN	0253-2786
卷号	39 期号:2 页码:397-405
摘要	Rice sheath blight disease, one of three most important diseases in rice, can lead to crop production loss seriously. However, the application of fungicides is an effective way to prevent rice from diseases. After being used for a period of time, the plant pathogenic fungi may develop resistance to chemical fungicide, so it is necessary to discover compounds with novel structures and further to address the problem of fungicide resistance. By employing the intermediate derivatisation method (IDM), twenty-five new phenylpyrazoloxyl propionic acid derivatives were designed and synthesized. The biological activities of title compounds were tested against Rhizoctonia solani and their structure-activity relationships (SAR) were discussed as well. The preliminary bioassay results displayed that some compounds exhibited an excellent fungicidal activity against Rhizoctonia solani, especially 24(1-(4-chlorophenyl)-1H-pyrazol-3-yl)oxy)-N-(4-nitrophenyl)propanamide ( 17 ) (EC50 =1.05 mg/L) and 24(1-(4-chlorophenyl)-1H-pyrazol-3-ypoxy)-N-(pyridin-2-yl)propanamide (22) (EC50 =1.02 mg/L) showing a comparable activity to the commercial contrast tebuconazole (EC50 =1.02 mg/L), and 24(1-(4-chlorophenyl)-1H-pyrazol-3-yl)oxy)-N-(3,4-dichlorophenyl)propanamide (20) (EC50 =0.95 mg/L) is a little more active than tebuconazole (EC50 =1.02 mg/L).
其他摘要	Rice sheath blight disease, one of three most important diseases in rice, can lead to crop production loss seriously. However, the application of fungicides is an effective way to prevent rice from diseases. After being used for a period of time, the plant pathogenic fungi may develop resistance to chemical fungicide, so it is necessary to discover compounds with novel structures and further to address the problem of fungicide resistance. By employing the intermediate derivatisation method (IDM), twenty-five new phenylpyrazoloxyl propionic acid derivatives were designed and synthesized. The biological activities of title compounds were tested against Rhizoctonia solani and their structure-activity relationships (SAR) were discussed as well. The preliminary bioassay results displayed that some compounds exhibited an excellent fungicidal activity against Rhizoctonia solani, especially 2-((1 -(4-chlorophenyl)-1H-pyrazol-3-yl)oxy)-N-(4-nitrophenyl)propanamide (17) (EC_(50)= 1.05 mg/L) and 2-((1 -(4-chlorophenyl)- 1H-pyrazol-3-yl)oxy)-N-(pyridin-2-yl)propanamide (22) (EC_(50)=1.02 mg/L) showing a comparable activity to the commercial contrast tebuconazole (EC_(50)=1.02 mg/L), and 2-((1 -(4-chlorophenyl)- 1H-pyrazol-3-yl)-oxy)-N-(3,4-dichlorophenyl)propanamide (20) (EC_(50)=0.95 mg/L) is a little more active than tebuconazole (EC_(50)= 1.02 mg/L).
关键词	phenylpyrazoloxyl propionic acid derivatives intermediate derivatization method fungicidal activity Rhizoctonia solani structure-activity relationship
收录类别	CSCD
语种	英语
资助项目	[Liaoning Provincal Science and Technology Plan Projects]
CSCD记录号	CSCD:6442607
引用统计
文献类型	期刊论文
条目标识符	http://ir.imr.ac.cn/handle/321006/153459
专题	中国科学院金属研究所
作者单位	中国科学院金属研究所
推荐引用方式 GB/T 7714	Yu Fuqiang,Guan Aiying,Sun Xufeng,et al. Design, Synthesis and Fungicidal Activity against Rhizoctonia solani of New Phenylpyrazoloxyl Propionic Acid Derivatives[J]. CHINESE JOURNAL OF ORGANIC CHEMISTRY,2019,39(2):397-405.
APA	Yu Fuqiang,Guan Aiying,Sun Xufeng,Li Huichao,&Li Xiaowu.(2019).Design, Synthesis and Fungicidal Activity against Rhizoctonia solani of New Phenylpyrazoloxyl Propionic Acid Derivatives.CHINESE JOURNAL OF ORGANIC CHEMISTRY,39(2),397-405.
MLA	Yu Fuqiang,et al."Design, Synthesis and Fungicidal Activity against Rhizoctonia solani of New Phenylpyrazoloxyl Propionic Acid Derivatives".CHINESE JOURNAL OF ORGANIC CHEMISTRY 39.2(2019):397-405.