Synthesis and anti-HBV evaluation of mono L-amino acid ester, mono non-steroid anti-inflammation drug carboxylic ester derivatives of acyclonucleoside phosphonates  

作　　者：Xiao-Zhong Fu Feng-Jie Jiang Yu Ou Sheng Fu Yu-Feng Cha Shun Zhang Zong-Yuan Liu Wen Zhou Ai-Min Wang Yong-Lin Wang 

机构地区：[1]School of Pharmacy,Guiyang Medical College,Engineering Research Center for the Development and Application of Ethnic Medicines and TCM,Ministry of Education [2]Provincial Key Laboratory of Pharmaceutics in Guizhou Province [3]Guiyang Women and Children’s Hospital and Health Institute

出　　处：《Chinese Chemical Letters》2014年第1期115-118,共4页中国化学快报（英文版）

基　　金：supported by the National Natural Science Foundation of China(Nos.20962004,81260473);Projects of Guizhou Science and Technology Department(Nos.2013-3031,2012-3013);Excellent Youth Scientific Talents Foundation of Guizhou(No.2013-45)

摘　　要：A series of mono L-amino acid ester, mono non-steroid anti-inflammation drug （NSAID）, carboxylic ester derivatives of acyclonucleoside phosphonates were prepared by using a ＂one pot synthesis＂ method and their in vitro anti-HBV activity were evaluated in HepG 2.2.15 cells. Compound 9a exhibited more potent anti-HBV activity and lower cytotoxicity than those of adefovir dipivoxil with IC50 and selective index （SI） values of 0.48μmol/L and 763.72, respectively.A series of mono L-amino acid ester, mono non-steroid anti-inflammation drug （NSAID）, carboxylic ester derivatives of acyclonucleoside phosphonates were prepared by using a ＂one pot synthesis＂ method and their in vitro anti-HBV activity were evaluated in HepG 2.2.15 cells. Compound 9a exhibited more potent anti-HBV activity and lower cytotoxicity than those of adefovir dipivoxil with IC50 and selective index （SI） values of 0.48μmol/L and 763.72, respectively.

关 键 词：Acyclonucleoside phosphonate Non-steroid anti-inflammation drug Anti-HBV activity 

分 类 号：TQ463[化学工程—制药化工]