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Synthesis and Bioactivity of Novel Sulfonate Scaffold-Containing Pyrazolecarbamide Derivatives as Antifungal and Antiviral Agents

文献类型： 外文期刊

作者： Lei, Zhi-Wei 1 ; Yao, Jianmei 2 ; Liu, Huifang 2 ; Ma, Chiyu 2 ; Yang, Wen 2 ;

作者机构： 1.Guizhou Univ, State Key Lab Breeding Base Green Pesticide & Agr, Key Lab Green Pesticide & Agr Bioengn, Minist Educ, Guiyang, Peoples R China

2.Guizhou Acad Agr Sci, Tea Res Inst, Guiyang, Peoples R China

关键词： pyrazolecarbamide; sulfonate; antifungal activity; antiviral activity; synthesis

期刊名称：FRONTIERS IN CHEMISTRY （ 影响因子：5.545； 五年影响因子：5.869 ）

ISSN： 2296-2646

年卷期： 2022 年 10 卷

页码：

收录情况： SCI

摘要： Novel pyrazolecarbamide derivatives bearing a sulfonate fragment were synthesized to identify potential antifungal and antiviral agents. All the structures of the key intermediates and target compounds were confirmed by nuclear magnetic resonance (NMR) and high-resolution mass spectrometry (HRMS). The single-crystal X-ray diffraction of the compound T22 showed that pyrazole carbamide is a sulfonate. The in vitro antifungal activities of the target compounds against Colletotrichum camelliae, Pestalotiopsis theae, Gibberella zeae, and Rhizoctonia solani were evaluated at 50 mu g/ml. Among the four pathogens, the target compounds exhibited the highest antifungal activity against Rhizoctonia solani. The compound T24 (EC50 = 0.45 mg/L) had higher antifungal activity than the commercial fungicide hymexazol (EC50 = 10.49 mg/L) against R. solani, almost similar to bixafen (EC50 = 0.25 mg/L). Additionally, the target compounds exhibited protective effects in vivo against TMV. Thus, this study reveals that pyrazolecarbamide derivatives bearing a sulfonate fragment exhibit potential antifungal and antiviral activities.

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