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樟脑酸基双酰肼化合物的合成及其抑菌活性

Synthesis and Antifungal Activity of Camphoric Acid-Based Diacylhydrazine Compounds

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【作者】 马献力李芳耀段文贵林桂汕陈乃源马媛

【Author】 MA Xian-li;LI Fang-yao;DUAN Wen-gui;LIN Gui-shan;CHEN Nai-yuan;MA Yuan;School of Chemistry and Chemical Engineering,Guangxi University;School of Pharmacy,Guilin Medical University;

【机构】 广西大学化学化工学院桂林医学院药学院

【摘要】 以樟脑酸为原料,经过脱水反应制备樟脑酸酐,再与芳酰肼发生N-酰化反应,合成得到10个樟脑酸基双酰肼化合物Ⅲa~Ⅲj。初步探索了合成条件,并利用FTIR、1HNMR、13CNMR和ESI-MS对目标产物进行结构表征。初步的生物活性测试表明,在50 mg/L质量浓度下,部分化合物表现出良好的抑菌活性,其中樟脑酸基烟酰肼Ⅲh对苹果轮纹病菌的抑制率高达96.3%,优于阳性对照嘧菌酯。

【Abstract】 Camphoric anhydride was prepared by using camphoric acid as raw materials. Then,ten novel camphoric acid-based diacylhydrazine compounds Ⅲ a ~ Ⅲ j were synthesized by the N-acylation reaction of camphoric anhydride with aromatic acylhydrazines. The synthetic conditions were investigated preliminarily and the target compounds were characterized by FTIR,1HNMR,13 CNMR and ESI-MS. The preliminary bioassay showed that,with the concentration of 50 mg / L,part of the title compounds exhibited good antifungal activity,in which compound camphoric acid-based nicotinoyl hydrazine Ⅲh had inhibition ratio of 96. 3% against Physalospora piricola( better than that of the positive control azoxystrobin).

【基金】 国家自然科学基金项目(31260164);广西高校科学技术研究重点项目(ZD2014098)~~
  • 【分类号】O623.752
  • 【被引频次】6
  • 【下载频次】266
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