Synthesis and Bioactivity Evaluation of Novel N-Pyridylpyrazolemethanamine Derivatives  

作　　者：HUA Xuewen WEI Wei ZHU Liangliang ZHOU Yunyun 

机构地区：[1]College of Agronomy, Liaocheng University, Liaocheng 252000, P. R. China [2]State Key Laboratory of Molecular Engineering of Polymers, Department of Macromolecular Science, Fudan University, Shanghai 200433, R R. China [3]Wuxi AppTee(Tianjin) Co., Ltd., Tianjin 300457, R R. China

出　　处：《Chemical Research in Chinese Universities》2018年第5期744-750,共7页高等学校化学研究（英文版）

基　　金：Supported by the National Natural Science Foundation of China（No.21502229）, the Natural Science Foundation of Shandong Province, China（No.ZR2017BC053） and the Doctoral Research Startup Foundation of Liaocheng University, China （No.318051625）.

摘　　要：To further explore the structure-activity relationship（SAR） of amide bridge moeity of anthranilic diamides derivatives, a series of N-pyridylpyrazole derivatives was designed, synthesized and their biological activities were evaluated. The chemical structures of novel target compounds were confirmed by 1H nuclear magnetic resonance （N-MR）, 13C NMR and elemental analyses（EA）. Bioassay results of insecticidal activity demonstrated that the target compound 6h displayed 70% lethality rate against oriental armyworms at 200 mg/L. Moreover, most compounds displayed moderate to excellent antifungicidal activities against Fusarium oxysporumf sp. cucumerinum, Cercospora arachidicola Hori, Botryosphaeria dothidea, Alternaria solani, Gibberella zeae and Phytophthora capsici at 50 mg/L In particular, compound 6e showed 61.5% and 92.3% inhibition rate against Cercospora arachidicola Hori and Botryosphaeria dothidea, which was superior to the commercial positive control Chlorothalonil. These results will provide a potential clue for exploring novel high-effective agrochemicals.To further explore the structure-activity relationship（SAR） of amide bridge moeity of anthranilic diamides derivatives, a series of N-pyridylpyrazole derivatives was designed, synthesized and their biological activities were evaluated. The chemical structures of novel target compounds were confirmed by 1H nuclear magnetic resonance （N-MR）, 13C NMR and elemental analyses（EA）. Bioassay results of insecticidal activity demonstrated that the target compound 6h displayed 70% lethality rate against oriental armyworms at 200 mg/L. Moreover, most compounds displayed moderate to excellent antifungicidal activities against Fusarium oxysporumf sp. cucumerinum, Cercospora arachidicola Hori, Botryosphaeria dothidea, Alternaria solani, Gibberella zeae and Phytophthora capsici at 50 mg/L In particular, compound 6e showed 61.5% and 92.3% inhibition rate against Cercospora arachidicola Hori and Botryosphaeria dothidea, which was superior to the commercial positive control Chlorothalonil. These results will provide a potential clue for exploring novel high-effective agrochemicals.

关 键 词：Anthranilic diamide Biological activity Antifungal agent 

分 类 号：TS202.3[轻工技术与工程—食品科学] O636.1[轻工技术与工程—食品科学与工程]