Synthesis of N-substituted dimethylmaleimides and their antifungal activities against Sclerotinia sclerotiorum
Synthesis of N-substituted dimethylmaleimides and their antifungal activities against Sclerotinia sclerotiorum
复制标题
N-取代二甲基马来酰亚胺的合成及其对核盘菌的抗真菌活性
DOI：
10.1007/s10340-012-0466-6
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发表时间：
2013-06-01
影响因子：
4.8
通讯作者：
Shen, Yinchu
中科院分区：
文献类型：
--
作者：
Shen, Zhenzhong;Fan, Yongxian;Shen, Yinchu
含有马来酰亚胺的天然和人工合成的化合物都具有良好的生物活性，尤其是抗真菌活性。为了研究二甲基马来酰亚胺的抗真菌活性，以2，3-二甲基马来酸酐和胺为原料，采用简便的合成方法合成了17个N-取代的二甲基马来酰亚胺。用菌丝生长速率法评价了这些化合物对核盘菌的抑菌活性。它们的最低抑菌浓度(MIC)为0.01~50.0mU g/m L，其中N-(2-苯并咪唑)-3，4-二甲基马来酰亚胺的最低抑菌浓度为0.01 m g/m L。这些化合物的结构和活性关系表明，N-取代基的疏水性与其抗真菌活性有关。与现有的抗真菌药物相比，大多数N-取代的二甲基马来酰亚胺对菌核病菌具有较好的防治活性，且毒性较低。
Compounds with maleimide, both natural and synthesized, have good biological activities, especially the antifungal activity. In order to investigate the antifungal activity of dimethylmaleimides, 17 N-substituted dimethylmaleimides were prepared from the reactions of 2,3-dimethyl maleic anhydride and amines using a facile synthetic method in this paper. These compounds were evaluated for antifungal activities against Sclerotinia sclerotiorum by the mycelium growth rate method. They exhibited minimum inhibitory concentrations (MICs) ranging from 0.01-50.0 mu g/mL, with N-(2-benzimidazole)-3,4-dimethylmaleimide being the most active one with an MIC of 0.01 mu g/mL. The structure and activity relationship on these compounds indicated that the hydrophobicity of the N-substituents is associated with their antifungal activity. Compared to current antifungals, most of N-substituted dimethylmaleimides have a perfect activity for S. sclerotiorum control and low toxicity.