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天然产物吩嗪-1-羧酸(PCA,申嗪霉素)及其衍生物吩嗪-1-甲酰肼具有独特的化学结构和优良的杀菌等生物活性,但均没有韧皮部输导性。本文以具有抑菌活性的吩嗪-1-羧酸和具有韧皮部输导性的马来酰肼为先导化合物,将马来酰肼中的双酰肼结构引入到吩嗪-1-羧酸中,设计、合成了17个新化合物,其结构均经过核磁共振氢谱、高分辨质谱及X-射线单晶衍射分析确证。初步生物活性测试表明:大部分目标化合物在50 mg/L下对水稻纹枯病菌Thanatephorus cucumeris表现出中等偏上的抑制活性,其中化合物6m的抑制率达92%。但输导性研究结果显示,目标化合物没有明显的韧皮部输导性。
The natural products phenazine-1-carboxylic acid (PCA, shenzhenmycin) and its derivatives phenazine-1-carboxylic acid hydrazide has a unique chemical structure and excellent biological activity such as sterilization, but no phloem conductivity. In this paper, phenazine-1-carboxylic acid with antibacterial activity and maleic hydrazide with phloem conductivity as the lead compound, the dihydrazide structure of maleic hydrazide was introduced into phenazine-1-carboxylic acid , 17 new compounds were designed and synthesized. Their structures were confirmed by 1H-NMR, high-resolution mass spectrometry and single crystal X-ray diffraction analysis. The preliminary bioassay showed that most of the target compounds exhibited moderately superior inhibitory activity against Thaniatus cucumeris at 50 mg / L, of which compound 6m had a 92% inhibition rate. However, conducting studies show that there is no significant phloem conductivity in the target compound.