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Synthesis and biological evaluation of Matijing-Su derivatives as potent anti-HBV agents. 2011
Jingying Qiu, and
Bixue Xu, and
Zhengming Huang, and
Weidong Pan, and
Peixue Cao, and
Changxiao Liu, and
Xiaojiang Hao, and
Baoan Song, and
Guangyi Liang
Center for Research and Development of Fine Chemicals of Guizhou University, Huaxi Road, Guiyang 550025, PR China.
A series of Matijing-Su (MTS, N-(N-benzoyl-l-phenylalanyl)-O-acetyl-L-phenylalanol) derivatives were synthesized and evaluated for their anti-hepatitis B virus (HBV) activity in 2.2.15 cells. The IC(50) of compounds 14a (0.71 μM), 13c (2.85 μM), 13b (4.37 μM), etc. and the selective index of 13g (161.01), 13c (90.45), 13a (85.09) etc. of the inhibition on the replication of HBV DNA were better than those of the positive control lamivudine (IC(50): 82.42 μM, SI: 41.59). Compounds 13o, 13p, and 16a also exhibited significant anti-HBV activity.
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