齐墩果酸肟醚类化合物的合成及杀菌活性

为了开发潜在的氨基葡萄糖-6-磷酸合成酶（GlmS）抑制剂和杀菌剂，设计并合成了30个齐墩果酸肟醚类化合物，其中29个为新化合物，其结构均经1H NMR、13C NMR和高分辨质谱确证。采用Elson-Morgan法和菌丝生长速率法，分别测定了目标化合物对GlmS的抑制活性和杀菌活性。结果表明:在0.35 mmol/L下，大部分目标化合物对GlmS表现出一定的抑制活性，其中，化合物A-01、A-02、A-04、C-04和C-05对GlmS的抑制率在30%左右；部分化合物在50 μg/mL下对油菜菌核病菌Sclerotinia sclerotiorum（Lib.）de Bary、番茄灰霉病菌Botrytis cinerea Pers. 和稻瘟病菌Pyricularia oryzae Cav. 具有较好的杀菌活性，其中，化合物A-01、A-02、A-04、A-05和B-02对油菜菌核病菌的抑制率在88%左右，具有进一步研究的价值。

Synthesis and fungicidal activities of the oleanolic acid oxime ethers

In order to develop potential glucosamine-6-phosphate synthase (GlmS) inhibitors and anti-fungal agents, 30 oleanolic acid oxime ethers were synthesized in an efficient way, and 29 of them were new compounds. The structures of all the synthesized compounds were characterized by 1H NMR, 13C NMR and HRMS. Preliminary studies based on the Elson-Morgan method and mycelial growth rate method indicated that, many compounds exhibited inhibitory activities against GlmS at the concentration of 0.35 mmol/L. And the inhibition rate of compounds A-01, A-02, A-04, C-04 and C-05 were about 30%. The original fungicidal activities results showed that some of the compounds exhibited good fungicidal activities to Sclerotinia sclerotiorum (Lib.) de Bary, Botrytis cinerea Pers. and Pyricularia oryzae Cav. at the concentration of 50 μg/mL. And the inhibition rate of compounds A-01, A-02, A-04, A-05 and B-02 against S. sclerotiorum were about 88%. These compounds will be further studied as potential antifungal lead compounds.