Citation: Xiao Zhong Fu, Sai Hong Jiang, Jian Xin, Yu She Yang, Ru Yun Ji. Design, synthesis and in vitro evaluation of L-amino acid esters prodrugs of acyclic nucleoside phosphonates as anti-HBV agent[J]. Chinese Chemical Letters, ;2007, 18(7): 817-819. doi: 10.1016/j.cclet.2007.05.013 shu

Design, synthesis and in vitro evaluation of L-amino acid esters prodrugs of acyclic nucleoside phosphonates as anti-HBV agent

a School of Pharmacy, Guiyang Medical College, Guiyang 550004, China;
b State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Shanghai Institute for Biological Sciences, Chinese Academy of Science, Shanghai 201203, China;
c Shanghai Fudan-Yueda Bio-Tech Co. Ltd., Shanghai 201203, China

Received Date: 8 January 2007

A series of novel L-amino acid esters prodrugs of acyclic nucleoside phosphonates was synthesized and their anti-HBV activity was evaluated in HepG22.2.15 cells. Compound 1d exhibited more potent anti-HBV activity and lower cytotoxicity than those of adefovir dipivoxil with EC₅₀ and CC₅₀ values of 0.207 μmol/L and 2530 μmol/L, respectively.
- Acyclic nucleoside phosphonates,
- L-Amino acid,
- Prodrug,
- Anti-HBV activity
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