Bioorganic & Medicinal Chemistry 2011-09-15

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

Jingying Qiu, Bixue Xu, Zhengming Huang, Weidong Pan, Peixue Cao, Changxiao Liu, Xiaojiang Hao, Baoan Song, Guangyi Liang

文献索引：Bioorg. Med. Chem. 19(18) , 5352-60, (2011)

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摘要

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.Copyright © 2011 Elsevier Ltd. All rights reserved.