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| Synthesis and Biologial Activities of Novel Magnolol -2-Azomethine Derivatives |
| MEI Fan1a,1b, ZHAI Ting1a,1b, ZHENG Nian1a,1b, LI Yan1a,1b, CHEN Yong1a,1c, LOU Zhao-wen1a,1b |
| a. Organic Chemical Materials Collaborative Innovation Center in Hubei; b. Chemistry and Chemical Engineering; c. College of Life Sciences, 1. Hubei University, Wuhan 430062, China |
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Abstract 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 substituted magnolol 2-azomethine derivatives were synthesized by reaction of the formylated magnolol with glycine, glutamic acid, arginine and sulfanilamide, respectively. The structures were characterized by UV-Vis, 1H 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 64 μmol·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.
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Received: 09 April 2015
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2016, Vol. 24 
