Studies on synthesis and antiviral activities of 5-substituted pyrimidine acyclic nucleoside phosphonate compounds on HBV

Key words: 
• 5-substituted pyrimidine /
• chemical synthesis /
• acyclic nucleotide /
• anti-HBV activity

Abstract: Objective :To study on synthesis and antiviral activities of 5-substituted pyrimidine acyclic nucleoside phosphonate compounds on HBV. Methods : Starting with substituted pyrimidine,we synthesized 8 firstly reported compounds 1a～1h.Preliminary pharmacological test was made on HBV. Results :TThe test results show the inhibitory rate of targeted compounds on HBsAg and HBeAg is normal,but 1d is higher than lamivudine. Conclusion :5-substituted pyrimidine acyclic nucleoside phosphonate compounds keep the normal activities on HBV and introduce long chain of chloroformate at N6 of pyrimidine shows better activity.