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A series of oleanolic acid derivatives were synthesized by diverse reactions, including the introduction of conjugated alkadiene and epoxy ring moieties formed by means of photosensitized oxidation. Eosin Y was used as photosensitizer during this process. Next the cytotoxicity of the products was evaluated on HepG2.2.15 cells to determine the appropriate treatment concentration for the subsequent experiments. Most of the  OA  derivatives exhibited anti-HBV antigens secretion activity in HepG2.2.15 cells. Among the tested compounds,  OA-4  (3.13 µg/mL) showed significant activity against the secretion of HBsAg, HBeAg, and HBV DNA replication with inhibitory ratios of 90.52% ± 1.78%, 31.55% ± 3.65%, and 94.57% ± 3.11% after 6 days, respectively. Besides,  OA-4  was further investigated in a duck model with DHBV infection. When  OA-4  was administered at a dosage of 500 mg/kg, the results revealed a significant inhibitory effects of DHBV at 19.94% ± 2.87%, 28.80% ± 3.62% and 29.25% ± 2.65% at days 5, 10, and 3 after the cessation of  OA-4  treatment, respectively. It’s worth noting that  OA-4  is superior to lamivudine in the inhibition of rebound of viral replication rate. The structure–activity relationships of  OA  derivatives had been preliminary discussed, which should be useful to explore further novel anti-HBV agents.

A Series of Oleanolic Acid Derivatives as Anti-Hepatitis B Virus Agents: Design, Synthesis, and in Vitro and in Vivo Biological Evaluation