Synthesis and Bioactivity Evaluation of Novel N-Pyridylpyrazolemethanamine Derivatives
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To further explore the structure-activity relationship(SAR) of amide bridge moeity of anthranilic diamides derivatives, a series of N-pyridylpyrazole derivatives was designed, synthesized and their biological activities were evaluated. The chemical structures of novel target compounds were confirmed by 1H nuclear magnetic resonance (NMR), 13C NMR and elemental analyses(EA). Bioassay results of insecticidal activity demonstrated that the target compound 6h displayed 70% lethality rate against oriental armyworms at 200 mg/L. Moreover, most compounds displayed moderate to excellent antifungicidal activities against Fusarium oxysporum f. sp. cucumerinum, Cercospora arachidicola Hori, Botryosphaeria dothidea, Alternaria solani, Gibberella zeae and Phytophthora capsici at 50 mg/L. In particular, compound 6e showed 61.5% and 92.3% inhibition rate against Cercospora arachidicola Hori and Botryosphaeria dothidea, which was superior to the commercial positive control Chlorothalonil. These results will provide a potential clue for exploring novel high-effective agrochemicals.
KeywordsAnthranilic diamide Biological activity Antifungal agent
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- Roditakis E., Steinbach D., Moritz G., Vasakis E., Stavrakaki M., Ilias A., García-Vidal L., Martínez-Aguirre M. D. R., Bielza P., Morou E., Silva J. E., Silva W. M., Siqueira H. A. A., Iqbal S., Troczka B. J., Williamson M. S., Bass C., Tsagkarakou A., Vontas J., Nauen R., Insect Biochemistry and Molecular Biology, 2017 80, 11CrossRefGoogle Scholar