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Short Paper | Regular issue | Vol 96, No. 8, 2018, pp.1453-1462
Published online, 26th July, 2018
DOI: 10.3987/COM-18-13944
Synthesis and Bioactivities Evaluation of Novel N-Pyridylpyrazole Derivatives with 1,2,3-Triazole and Quinazolin-4(3H)-one Substructures

Wei Wei, Liangliang Zhu, Yunyun Zhou,* and Zhengming Li*

*State Key Laboratory of Molecular Engineering of Polymers, Department of Macromolecular Science, Fudan University, Songhu Road No. 2005, Shanghai, 200433, China

Abstract

Two series of N-pyridylpyrazole derivatives containing 1,2,3-triazole and quinazolin-4(3H)-one substructures were designed and synthesized. In total, 18 novel compounds were prepared, and all compounds were characterized by 1H NMR, 13C NMR and elemental analysis (EA). Preliminary bioassay results revealed that a few of new compounds with quinazolin-4(3H)-one moiety exhibited good insecticidal activity against the oriental armyworm (Mythimna separata). In addition, the compounds Ia-h with 1, 2, 3-triazole moiety showed broad-spectrum antifungal activities against Fusarium oxysporum f.sp.cucumerinum, Cercospora arachidicola Hori, Botryosphaeria dothidea, Alternaria solani, Gibberella zeae and Phytophthora capsici at 50 μg/mL concentration. The EC50 values of Ib and If against Botryosphaeria dothidea were 13.9 and 11.0 μg/mL, respectively, which were comparable to Chlorothalonil. These results indicated the potential application of N-pyridylpyrazole derivatives as fungicide in further study.