Design, synthesis, and fungicidal activity of novel 1,3,4-oxadiazole derivatives

作     者：Fuqiang Yu Aiying Guan Mengru Li Lan Hu Xiaowu Li 

作者机构：Department of Materials Physics and Chemistry School of Material Science and Engineering and Key Laboratory for Anisotropy and Texture of MaterialsMinistry of Education Northeastern University State Key Laboratory of the Discovery and Development of Novel Pesticide Shenyang Sinochem Agrochemicals R&D Co.Ltd. 

出 版 物：《Chinese Chemical Letters》 (中国化学快报（英文版）)

年 卷 期：2018年第29卷第6期

页      面：915-918页

核心收录：

学科分类：090403[农学-农药学(可授农学、理学学位）] 09[农学] 0904[农学-植物保护] 

基　　金：financially supported partially by the Open Foundation of Key Laboratory for Anisotropy and Texture of Materials  Ministry of Education  Northeastern University  China (No. ATM20170001) 

主　　题：1,3,4-Oxadiazole derivatives Intermediate derivatization method Rice sheath blight Sorghum anthracnose Structure-activity relationship 

摘      要：Employing the intermediate derivatization method（IDM）, twenty novel 1,3,4-oxadiazole derivatives containing arylpyrazoloxyl moiety were designed and synthesized. The structures of the title compounds were identified by1 H NMR,13 C NMR, MS and elemental analyses, compound 4 was further identified by single-crystal X-ray diffraction. Antifungal activities against rice sheath blight（RSB） and sorghum anthracnose（SA） were evaluated by the mycelium linear growth rate method. Compounds 4, 16 and 20 displayed significant activities against RSB（EC50= 0.88 mg/L, 0.91 mg/L and 0.85 mg/L, respectively）,higher than the reference tebuconazole; While compound 3 exhibited higher activity against SA（EC50= 1.03 mg/L）, equal to commercial pyraclostrobin（EC50= 1.06 mg/L）. The study showed that compound 20 is a promising fungicide for further development.