新型脱氢枞胺衍生物的合成及其抗自由基活性

Synthesis and Anti-free Radical Activities of Several Novel Derivatives of Dehydroabietylamine

通过不同的方法在脱氢枞胺中引入酰腙、没食子酸、肟、异烟基等对清除自由基有效果的基团,设计合成了几种新型的脱氢枞胺衍生物.利用1H NMR,13C NMR,IR和HRMS对所有合成的化合物进行了结构表征.测试了所合成的化合物对清除超氧阴离子(O2-)和二苯代苦味酰基自由基(DPPH·)的活性,其中N-(3,4,5-三羟基苯甲酰基)-脱氢枞胺(6)对O-2的抑制率达到38.18%,是常用抗氧化药物Vc(18.35%)的两倍以上;对(DPPH·)的半数抑制浓度为0.002×103 mg/L,远优于Vc(0.236×103 mg/L).

A series of novel derivatives of dehydroabietylamine were synthesized by introducing some groups with good free radical scavenging activities into the dehydroabietylamine, such as hydrazone, gallic acid, oxime and isoniazid. Structures of the synthesized compounds were characterized by IR, 1H NMR, 13C NMR, MS and HRMS techniques. All the compounds were tested the ability on scavenging superoxide anion radical （O2） and 1,1-dipheny-2-picrylhydrazyl （DPpHo）. The results indicate that the inhibitory rate of 02 by （6） （38.18%） is twice as much as that of Vc （18.35%）, and its capacity on scaveng- ing DPPH, （IC50=0.002 ×10^3 mg/L） is much better than Vc （IC50=0.236 × 10^3 mg/L.