Synthesis and anti-hepatitis B virus activities of Matijin-Su derivatives

A series of Matijin-Su [MTS,N-(N-benzoyl-L-phenylalanyl)-O-acetyl-L-phenylalanol] derivatives were synthesized and evaluated for their abilities to inhibit the replication of hepatitis B virus(HBV) DNA in HepG2 2.2.15 cells.Compounds 5e (IC₅₀:10.67 μmol/L,SI:47.26), 4c (IC₅₀:11.09 μmol/L,SI:15.03), 4b (IC₅₀:19.75 μmol/L,SI:4.74), 5b (IC₅₀:59.55 μmol/L,SI:3.00) and 5a (IC₅₀:77.69 μmol/L,SI:5.81) exhibited significant inhibitory activity against the replication of HBV DNA in HepG2 2.2.15 cells,and were more potent than the positive control lamivudine(IC₅₀:82.42 μmol/L,SI:41.59).Compound 5e (IC₅₀:1.31 μmol/L,SI:326.31) showed the most potency in vitro anti-HBV activity within all the tested compounds,and could be a potent HBV inhibitor with high selectivity index.