Synthesis and Biological Activity of Benzamides Substituted with Pyridine-Linked 1,2,4-Oxadiazole

被引:16
作者
Yang, Sen [1 ]
Tian, Xiao-Yu [1 ]
Ma, Tian-Yang [1 ]
Dai, Li [1 ]
Ren, Chao-Li [1 ]
Mei, Jun-Chang [1 ]
Liu, Xing-Hai [1 ]
Tan, Cheng-Xia [1 ]
机构
[1] Zhejiang Univ Technol, Coll Chem Engn, Hangzhou 310014, Peoples R China
来源
MOLECULES | 2020年 / 25卷 / 15期
关键词
amide compound; fungicidal activity; insecticidal activity; 1; 2; 4-oxadiazole; synthesis; NEMATOCIDAL ACTIVITY; DERIVATIVES; DOCKING; ANALOGS; DESIGN; SAR;
D O I
10.3390/molecules25153500
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
To find pesticidal lead compounds with high activity, a series of novel benzamides substituted with pyridine-linked 1,2,4-oxadiazole were designed by bioisosterism, and synthesized easily via esterification, cyanation, cyclization and aminolysis reactions. The structures of the target compounds were confirmed by(1)H-NMR,C-13-NMR and HRMS. The preliminary bioassay showed that most compounds had good larvicidal activities against mosquito larvae at 10 mg/L, especially compound7a, with a larvicidal activity as high as 100%, and even at 1 mg/L was still 40%; at 50 mg/L, all the target compounds showed good fungicidal activities against the eight tested fungi. Moreover, compound7hexhibited better inhibitory activity (90.5%) than fluxapyroxad (63.6%) againstBotrytis cinereal. Therefore, this type of compound can be further studied.
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页数:12
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