SYNTHESIS, ANTIFUNGAL ACTIVITY AND QSAR OF NOVEL PYRAZOLE AMIDES AS SUCCINATE DEHYDROGENASE INHIBITORS

被引：9
作者：
Du, Shijie [1 ]
Li, Zhonghao [2 ]
Tian, Zaimin [2 ]
Xu, Lu [1 ]
机构：
[1] Tongren Univ, Coll Mat & Chem Engn, Tongren 554300, Peoples R China
[2] Hebei North Univ, Coll Anim Sci & Technol, Zhangjiakou 075131, Peoples R China
来源：
HETEROCYCLES | 2018年 / 96卷 / 01期
关键词：
DERIVATIVES; REDUCTION;
D O I：
10.3987/COM-17-13826
中图分类号：
O62 [有机化学];
学科分类号：
070303 ; 081704 ;
摘要：
We design and synthesize a series of novel pyrazole amides based on the commercialized fungicides and our previous work. The antifungal activity was tested in vitro by mycelial growth inhibition assay. The results show that all the compounds are of antifungal activities against the tested fungi at different levels. Among them, N-(2-(7-bromo-5-chloro-1H-indazol-1-yl)phenyl)-3-(difluoromethyl)-1-methyl-1H-pyrazole-4-carboxamide (Vk) exhibited higher antifungal activity than boscalid against two fungi. Molecular docking study revealed that the carbonyl oxygen atom of Vk forms two hydrogen bonds toward the hydroxyl hydrogens of TYR58 and TRP173.
引用
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页码：74 / 85
页数：12
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