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

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个新型樟脑酸基双酰肼化合物3a～3j。初步探索了合成条件，并利用FT-IR、1H NMR、13C NMR和ESI-MS等多种手段对目标产物作了结构表征。初步的生物活性测试表明，在50 mg/L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3h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 starting material and acetic anhydride as dehydrating agent. Then, ten novel camphoric acid-based diacylhydrazine compounds 3a～3j were synthesized by the N-acylation reaction of camphoric anhydride with aromatic acylhydrazines. The synthetic conditions were investigated preliminarily. The target compounds were characterized by means of FT-IR, 1H NMR, 13C NMR and ESI-MS techniques. The preliminary bioassay showed that, at the concentration of 50 mg/L, part of the title compounds exhibited good fungicidal activity, in which compound camphoric acid-based nicotinoyl hydrazine 3h had inhibition ratio of 96.3% against Physalospora piricola (better than that of the positive control azoxystrobin).