2. Academic Validation
  3. Synthesis and biological evaluation of Matijing-Su derivatives as potent anti-HBV agents

Synthesis and biological evaluation of Matijing-Su derivatives as potent anti-HBV agents

  • Bioorg Med Chem. 2011 Sep 15;19(18):5352-60. doi: 10.1016/j.bmc.2011.08.001.
Jingying Qiu 1,  Bixue Xu,  Zhengming Huang,  Weidong Pan,  Peixue Cao,  Changxiao Liu,  Xiaojiang Hao,  Baoan Song,  Guangyi Liang
Affiliations

Affiliation

  • 1 Center for Research and Development of Fine Chemicals of Guizhou University, Huaxi Road, Guiyang 550025, PR China.
PMID: 21872478 DOI: 10.1016/j.bmc.2011.08.001
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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