中文摘要：

以阿德福韦为原料,设计并合成了6个新型结构的阿德福韦单L-氨基酸酯、单胆酸酯衍生物1a~1f,通过ESIMS、HRMS、^1H NMR和^13C NMR确证结构。采用Hep G2.2.15细胞和大鼠原代肝细胞考察了化合物1a~1f的抗HBV活性和肝细胞摄取情况。结果表明,阿德福韦膦酸基上引入胆酸酯结构片段能够明显提高化合物被肝细胞摄取的能力,同时提高其抗病毒活性。化合物1c的抗病毒活性与肝细胞摄取能力最好,值得进一步研究。

英文摘要：

Six L-amino acid and bile acid ester derivatives of adefovir （1a-1f） were prepared from adefovir by one pot synthesis method. Their structures were confirmed by ESI-MS, HRMS, ^1H NMR, and ^13C NMR. The anti-HBV activitives and hepatocyte.uptake abilities in HepG2.2.15 cells and rat primary hepatocytes of la--lf were investigated, respectively. The results indicated that incorporation of bile acid fragment to adefovir could significantly improve the hepatocyte uptake abilities, meanwhile increasing the anti-HBV activities. Compound lc with the highest antiviral activity and hepatocyte uptake ability would be worthy of further studies.