SYNTHESIS AND BIOACTIVITIES EVALUATION OF NOVEL N-PYRIDYLPYRAZOLE DERIVATIVES WITH 1,2,3-TRIAZOLE AND QUINAZOLIN-4(3H)-ONE SUBSTRUCTURES

摘要

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 H-1 NMR, C-13 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 [mu g/mL concentration. The EC50 values of Ib and If against Botryosphaeria dothidea were 13.9 and 11.0 mu g/mL, respectively, which were comparable to Chlorothalonil. These results indicated the potential application of N-pyridylpyrazole derivatives as fungicide in further study.