Design, synthesis and in vitro evaluation of mono (2, 2, 2-trifluoroethyl) esters, mono l-amino acid ester prodrugs of acyclic nucleoside phosphonates as anti-HBV agents |
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| Authors: | Xiao Zhong Fu Yu Ou Jan Xin Yu She Yang |
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| Institution: | a School of Pharmacy, Guiyang Medical College, Guiyang 550004, China;b Shanghai Fudan-Yueda Bio-Tech Co., Ltd., Shanghai 201203, China;c State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Shanghai Institute for Biological Sciences, Chinese Academy of Science, Shanghai 201203, China |
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| Abstract: | A series of novel mono (2, 2, 2-trifluoroethyl) esters, mono l-amino acid ester prodrugs of acyclic nucleoside phosphonates was synthesized and their in vitro anti-HBVactivity was evaluated in HepG 2 2.2.15 cells. Compound 1d exhibited more potent anti-HBV activity and lower cytotoxicity than those of adefovir dipivoxil and alamifovir (MCC-478) with EC50 and CC50 values of 0.01 μmol/L and >8000 μmol/L respectively. |
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| Keywords: | Acyclic nucleoside phosphonates l-Amino acid" target="_blank">l-Amino acid Prodrug |
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