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Published on: December 21, 2019
Synthesis and biological evaluation of Matijing-Su derivatives as potent anti-HBV agents
Jingying Qiu1, Bixue Xu, Zhengming Huang
1Center for Research and Development of Fine Chemicals of Guizhou University, Huaxi Road, Guiyang 550025, PR China.
Abstract:
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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