新型厚朴酚2-甲亚胺衍生物的合成及其生物活性

以厚朴酚为原料，通过Reimer-Tiemann法，在其苯环羟基邻位引入甲酰基后，分别与甘氨酸、谷氨酸、精氨酸及对氨基苯磺酰胺反应合成了4个单取代、1个二取代新型厚朴酚2-甲亚胺衍生物(3a~3d和4)，其结构经UV-Vis, ¹H NMR， IR， MS和元素分析表征。生物活性研究结果表明： 2-(N-甘氨酸)-厚朴酚甲亚胺(3a)对成肌细胞的毒性较大；2-［N-(4-氨磺酰苯基)］-厚朴酚甲亚胺(3d)浓度为64 μmol·L^-1时，对CYP2D6和CYP1A2的抑制率分别为42.9%和36.8%。

Synthesis and Biologial Activities of Novel Magnolol 2-Azomethine Derivatives

The formoxyl was introduced into the ortho-position of magnolol hydroxy by the Reimer-Tiemann method using magnolol as the raw material.Four novel mono-substituted and one bis substitu-ted magnolol 2-azomethine derivatives were synthesized by reaction of the formylated magnolol with gly-cine, glutamic acid, arginine and sulfanilamide, respectively.The structures were characterized by UV-Vis, 1 H NMR, IR, MS and elemental analysis.The myoblast cell toxicity and the effects on CYPs in liver microsomes in vitro human were investigated.The results showed that 2-( N-glycine)-magnolol azomethine(3a) exhibited certain tomyoblasts toxicity.At 64μmol· L-1 , the inhibition rate of 2- N-(4-sulfamoyl-phenyl)]-magnolol azomethine(3d) on CYP2D6 and CYP1A2 was 42.9%and 36.8%, respectively.