Citation: Peng Lu, Sai Hong Jiang, Jiang Xia Liu, Yu She Yang, Ru Yun Ji. Design,synthesis and anti-HBV activity of novel bis(trifluoroethyl)phosphonomethyl ether derivatives of acyclovir[J]. Chinese Chemical Letters, ;2009, 20(5): 507-510. doi: 10.1016/j.cclet.2008.12.057 shu

Design,synthesis and anti-HBV activity of novel bis(trifluoroethyl)phosphonomethyl ether derivatives of acyclovir

a State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Shanghai Institute for Biological Sciences, Chinese Academy of Science, Shanghai 201203, China;
b Fudan University, Shanghai 200032, China

Received Date: 10 November 2008

A series of novel bis(trifluoroethyl) phosphonomethyl ether derivatives of acyclovir was synthesized and their in vitro anti-HBV activity was evaluated in HepG2 2.2.15 cells. In contrast to acyclovir, most of the described phosphonates emerged as potent inhibitors of HBV replication. Especially, the most active compound 11 with IC₅₀ value of 2.92 mmol/L was 33 times more potent than acyclovir with IC₅₀ value of 100 mmol/L.
- Acyclovir,
- Phosphonate,
- Anti-HBV activity
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