Citation: Yu Fuqiang, Guan Aiying, Li Mengru, Hu Lan, Li Xiaowu. Design, synthesis, and fungicidal activity of novel 1, 3, 4-oxadiazole derivatives[J]. Chinese Chemical Letters, ;2018, 29(6): 915-918. doi: 10.1016/j.cclet.2018.01.050 shu

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

Yu Fuqiang ^a,b ,
Guan Aiying ^b,, ,
Li Mengru ^b ,
Hu Lan ^b ,
Li Xiaowu ^a,,

a.
Department of Materials Physics and Chemistry, School of Material Science and Engineering, and Key Laboratory for Anisotropy and Texture of Materials, Ministry of Education, Northeastern University, Shenyang 110819, China
b.
State Key Laboratory of the Discovery and Development of Novel Pesticide, Shenyang Sinochem Agrochemicals R & D Co., Ltd., Shenyang 110021, China

Corresponding author: Guan Aiying, guanaiying@sinochem.com Li Xiaowu, xwli@mail.neu.edu.cn
Received Date: 4 December 2017
Revised Date: 22 January 2018
Accepted Date: 24 January 2018
Available Online: 7 June 2018

Figures(3)

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 by ¹H NMR, ¹³C 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.
- 1, 3, 4-Oxadiazole derivatives,
- Intermediate derivatization method,
- Rice sheath blight,
- Sorghum anthracnose,
- Structure-activity relationship
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