Synthesis and biological evaluation of novel pyrazole carboxamide with diarylamine-modified scaffold as potent antifungal agents |
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Authors: | Xiao-Xiao Zhang Hong Jin Yuan-Jie Deng Xu-Heng Gao Yong Li Yong-Tian Zhao Ke Tao Tai-Ping Hou |
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Institution: | a Key Laboratory of Bio-Resource and Eco-environment of Ministry of Education, College of Life Sciences, Sichuan University, Chengdu 610064, China;
b College of Chemistry, Sichuan University, Chengdu 610064, China |
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Abstract: | Twenty-seven novel pyrazole carboxamides with diarylamine-modified scaffold were designed, synthesized and characterized in detail via 1H NMR, 13C NMR, IR and ESI-HRMS. Preliminary bioassays showed that some of the target compounds exhibited good antifungal activity against Rhizoctonia solani, Rhizoctonia cerealis and Sclerotinia sclerotiorum. Among them, compound 9c-7 exhibited the highest antifungal activities against R. solani, R. cerealis and S. sclerotiorum in vitro with IC50 values of 0.013, 1.608 and 1.874 μg/mL, respectively. Notably, compound 9c-7 still presented the highest fungicidal activities against R. solani in vivo with an IC50 value of 22.21 μg/mL. Molecular docking simulation results reveal that compound 9c-7 binds well to the hydrophobic pockets of the receptor protein succinate dehydrogenase. This study suggests that compound 9c-7 could act as a potential fungicide to be used for further optimization. |
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Keywords: | Pyrazole carboxamide Synthesis Antifungal activities Diarylamine |
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