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  

作　　者：Xiao Zhong Fu Yu Ou Jan Xin Yu She Yang 

机构地区：[1]School of Pharmacy,Guiyang Medical College,Guiyang 550004,China [2]Shanghai Fudan-Yueda Bio-Tech Co.,Ltd.,Shanghai 201203,China [3]State Key Laboratory of Drug Research,Shanghai Institute of Materia Medica,Shanghai Institute for Biological Sciences, Chinese Academy of Science,Shanghai 201203,China

出　　处：《Chinese Chemical Letters》2011年第12期1387-1390,共4页中国化学快报（英文版）

基　　金：supported by the grants from the National Natural Science Foundation of China(No.20962004);the Provincial Social Development Foundation of Guizhou,China(No.QKHSYZ[2009]3081);Provincial Special Assistant Foundation for High-level Talents of Guizhou,China(No.TZJF-2009-36);Science and Technology Foundation of Guizhou Province,China(No.QKHJZ[2008]2140)

摘　　要：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 EC_（50） and CC_（50） values of 0.01μmol/L and 8000μmol/L respectively.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 EC_（50） and CC_（50） values of 0.01μmol/L and 8000μmol/L respectively.

关 键 词：Acyclic nucleoside phosphonates L-Amino acid PRODRUG 

分 类 号：TQ453.22[化学工程—农药化工] TQ463.54