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A series of Matijing-Su (MTS,N-(N-benzoyl-L-phenylalanyl)-O-acetylL-phenylalanol) derivatives were synthesized and evaluated for their abilities to inhibit the replication of hepatitis B virus (HBV) DNA in HepG22.2.15 cells.Compounds 5r (IC50:1.31 μM,SI:326.31),5f (IC50:6.64 μM,SI:61.72),5a (IC50:6.87 μM,SI:42.74),5d (IC50:8.24 μM,SI:58.68) and 5h (IC50:10.28 μM,SI:47.21) etc.exhibited significant inhibitory on the replication of HBV DNA in 2.2.15 cells,which were better than those of the positive control lamivudine (IC50:82.42 μM,SI:41.59).