取代吲哚-3-甲醛类化合物抑菌活性研究

Antifungal Activities of Substituted Indole-3-carboxaldehyde Derivatives

拓宽取代吲哚-3-甲醛类化合物在抑制植物病原真菌活性的应用范围。首先通过Vilsmeier-Haack反应制备得到取代吲哚-3-甲醛类化合物（Ⅰ-Ⅴ）;采用菌丝生长速率法分别测定化合物对5种常见植物病原真菌的室内毒力。化合物Ⅰ-化合物Ⅴ对所测5种病原真菌均表现出不同程度的毒力。其中化合物5-硝基-3-醛基吲哚（Ⅳ）和5-氰基-3-醛基吲哚（Ⅴ）对油菜菌核病菌表现出高于霉灵的活性,其相对毒力分别是霉灵的325倍和1.86倍。

Five substituted indole-3-carboxaldehyde derivatives（Ⅰ-Ⅴ） were synthesized via the Vilsmeier-Haack reaction,and their antifungal activities against five kinds of common plant pathogenic fungi were investigated by mycelium growth rate method.A preliminary structure-activity relationship（SAR） was also studied.Compounds Ⅰ-Ⅴshowed different antifungal activities on five kinds of plant pathogenic fungi.5-Nitro-3-formylindole（Ⅳ） and5-cyano-3-formylindole（Ⅴ） exhibited strong potent activities against Sclerotinia sclerotiorum,the relative toxicity of Ⅳand Ⅴ were 325 times and 1.86 times higher than that of hymexazol,respectively.