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

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。

Camphorlc anhydride was prepared by using camphoric acid as raw materials. Then, ten novel camphoric acid-based diacylhydrazine compounds Ⅲ a ～Ⅲj 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 Ⅲ h had inhibition ratio of 96.3% against Physalospora piricola （better than that of the positive control azoxystrobin）.