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Paper | Regular issue | Vol 96, No. 1, 2018, pp.74-85
Published online, 5th December, 2017
DOI: 10.3987/COM-17-13826
■ Synthesis, Antifungal Activity and QSAR of Novel Pyrazole Amides as Succinate Dehydrogenase Inhibitors

Shijie Du, Zhonghao Li, Zaimin Tian, and Lu Xu*

*College of Material and Chemical Engineering, Tongren University, Tongren, 554300, China

Abstract

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.