| 房嘉华,王亚虎,赵恩崎,辛鸿玉,金雪微,刘鑫垚,景云荣.化学通报,2025,88(5):552-558. |
| 吡唑酰胺类衍生物的合成及抑菌活性研究 |
| Synthesis and Antibacterial Activity of Pyrazolamide Derivatives |
| 投稿时间：2024-12-19 修订日期：2025-02-09 |
| DOI： |
| 中文关键词: 吡唑酰胺衍生物 小麦赤霉菌 氟唑菌酰羟胺 抑菌活性 琥珀酸脱氢酶抑制剂 |
| 英文关键词:Pyrazolamide derivatives, Fusarium graminearum, Pydiflumetofen, Antibacterial activity, Succinate dehydrogenase inhibitor |
| 基金项目:黑龙江省教育厅基础科研业务项目(1451MSYYB002,1452TD009)和牡丹江师范学院校级项目(QN2021001)资助 |
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| 中文摘要: |
| 本文合成一系列吡唑酰胺类衍生物针对4种植物病原菌的抑菌活性进行研究。以不同取代的吡唑羧酸与不同芳环取代的脂肪胺进行酰胺缩合,制备得到一系列结构新颖的吡唑酰胺类衍生物,目标化合物的结构经质谱和核磁确证。采用菌丝生长速率法考察目标化合物针对4种不同植物病原菌的体外抑菌活性,筛选出抑菌活性高且具有广谱抑菌活性的候选化合物BX3-3。通过扫描电镜观察经BX3-3(0.05 μg/mL)处理过的小麦赤霉菌的菌丝表面形态发生显著改变,测定其针对琥珀酸脱氢酶(SDH)具有良好的抑制作用,IC50为0.051 μg/mL,与阳性对照氟唑菌酰羟胺相当。 |
| 英文摘要: |
| This study synthesized a series of pyrazolamide derivatives and systematically investigated their antibacterial activities against four plant pathogens. A novel array of pyrazolamide derivatives was prepared through amide condensation between substituted pyrazole carboxylic acids and aromatic ring-modified fatty amines. Structural confirmation of the target compounds was achieved using mass spectrometry (MS) and nuclear magnetic resonance (NMR) analyses. Antibacterial efficacy was evaluated using the mycelial growth rate method against four phytopathogens, leading to the identification of compound BX3-3 as a potent broad-spectrum antibacterial candidate. Scanning electron microscopy (SEM) revealed significant morphological alterations in fusarium graminearum hyphae following treatment with BX3-3 (0.05 mg/L). Enzymatic assays demonstrated that BX3-3 exhibits potent inhibitory activity against succinate dehydrogenase (SDH), with an IC50 value of 0.051 mg/L, comparable to the commercial fungicide pydiflumetofen. |
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