含苯基吡啶基团的肟醚乙酸酯类化合物的合成与抑菌活性

    Synthesis and fungicidal activity of novel methoximinoacetates containing phenylpyridine moieties

    • 摘要: 以3-羟基苯硼酸和取代含溴吡啶为原料,经Suzuki偶联和亲核取代两步反应合成了24个未见报道的含苯基吡啶基团的肟醚乙酸酯类化合物,其结构均通过1H NMR、ESI-MS和IR确证。初步生物活性测定结果表明,大部分目标化合物具有一定的抑菌活性,其中化合物 5i、 5r、 5t 在 50 mg/L下对黄瓜霜霉病菌的抑制率达到80%。说明此类化合物具有作为杀菌剂先导进行进一步结构优化的潜力。

       

      Abstract: Twenty four novel methoximinoacetate compounds containing phenylpyridine moieties were synthesized from (3-hydroxyphenyl)boric acid and substituted bromopyridines via Suzuki cross-coupling reaction and nucleophilic substitution. The structures of all compounds were confirmed by H NMR, ESI-MS and IR. Bioactivity tests showed that most of the compounds have moderate to good fungicidal activity and compounds 5i , 5r and 5t exhibited more than 80% inhibition against Pseudoperonospora cubensis at 50 mg/L, which means that the title compounds are potential as the fungicidal lead compounds.

       

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