The anti-HBV studies of a novel series of acyclic pyrimidine nucleoside analogs.

摘要

Presently, there are over 350 million chronic carriers of the hepatitis B virus (HBV). Chronic HBV infections lead to cirrhosis, liver failure, and hepatocellular carcinoma. Currently, lamivudine and adefovir are the most effective treatments for chronic HBV. However, viral rebound after the cessation of therapy and drug resistance upon continuous use are the two most significant limitations. Therefore, there is an increasing need for the development of novel antiviral treatments to augment the therapy, to avoid the emergence of drug resistance, or to use against the already established mutant forms. The aim of this project is to investigate two novel series of acyclic pyrimidine nucleoside analogs possessing various C-5 and/or C-6 substituents on the base moiety. It is our objective to synthesize and determine their anti-HBV effects, and establish the structure activity relationships (SARs) of these compounds, in the hopes of providing a possible novel treatment option.