Chinese Journal of Organic Chemistry >
Synthesis and Anti-hepatitis B Virus Activities of Matijin-Su Derivatives with Potential for Hepatic Targeting
Received date: 2015-05-07
Revised date: 2015-06-08
Online published: 2015-06-19
Supported by
Project supported by the National Natural Science Foundation of China (No. 81360472) and the Western Light Talent Culture Project (2014).
To improve the concentration in liver lesion tissue and increase the anti-hepatitis B virus (HBV) activity of Matijin-Su [N-(N-benzoyl-l-phenylalanyl)-O-acetyl-L-phenylalanol, MTS] derivatives, five galactosyl derivatives of MTS with potential for hepatic targeting were synthesized and their structures were confirmed by 1H NMR, 13C NMR, 1H-1H COSY, HMQC and ESI-MS. The anti-HBV activities of those compounds were evaluated in HepG2 2.2.15 cells. The screening results showed that all target compounds had inhibitory effect on HBV DNA replication in HepG2 2.2.15 cells in a dose-effect relationship.
Yuan Jie , Liu Qingchuan , Xu Guangcan , Hu Zhanxing , Liang Guangping , Huang Zhengming , Liu Changxiao , Liang Guangyi , Xu Bixue . Synthesis and Anti-hepatitis B Virus Activities of Matijin-Su Derivatives with Potential for Hepatic Targeting[J]. Chinese Journal of Organic Chemistry, 2015 , 35(10) : 2176 -2183 . DOI: 10.6023/cjoc201505011
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