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

  • Bioorg Med Chem. 2009 Apr 15;17(8):3118-25. doi: 10.1016/j.bmc.2009.03.003.
Bixue Xu  1 ,  Zhengming Huang ,  Changxiao Liu ,  Zegui Cai ,  Weidong Pan ,  Peixue Cao ,  Xiaojiang Hao ,  Guangyi Liang
Affiliations
  • 1. The Key Laboratory of Chemistry for Natural Products of Guizhou Province and Chinese Academy of Sciences, 202 Shachong South Road, Guiyang 550002, PR China.
PMID: 19307124 DOI: 10.1016/j.bmc.2009.03.003
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.