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

Bioorganic & Medicinal Chemistry
2009.0

Abstract

A series of derivatives of Matijing-Su (MTS, N-(N-benzoyl-L-phenylalanyl)-O-acetyl-L-phenylalanol) was synthesized and evaluated for their anti-hepatitis B virus (HBV) activities in 2.2.15 cells. The IC(50) of compounds 9c (1.40 microM), 9g (2.33 microM) and 9n (2.36 microM), etc. and the selective index of 9n (45.93) of the inhibition on the replication of HBV DNA were higher than those of the positive control lamivudine [41.59, (IC(50): 82.42 microM)]. Compounds 11d, 12a and 12e also exhibited significant anti-HBV activities.

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