Abstract
In order to explore novel natural product-based anti-oomycete and anti-fungal agents, fifteen aminoguanidine derivatives of paeonol sulfonate (5a-o) were designed and synthesized , and their structures were confirmed by 1H NMR, 13C NMR, HRMS, and melting point. The stereochemical configurations of compounds 5i and 5j have been confirmed by single-crystal X-ray diffraction. In addition, the anti-oomycete and anti-fungal activities of these target compounds against two serious agricultural diseases, Phytophthora capsici and Fusarium graminearum were evaluated by mycelial growth rate method. Among all tested compounds, 1) Four compounds 5e, 5f, 5g, and 5o exhibited promising anti-oomycete against P. capsici, with median effective concentration (EC50) values of 4.27, 9.20, 4.77, and 6.94 mg/L, respectively. 2) Compound 5 g displayed promising anti-fungal against F. graminearum, with an EC50 value of 17.75 mg/L. The results showed that the introduction of aminoguanidine active groups in the carbonyl position of paeonol sulfonate could enhance its activity against plant pathogens.
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