摘要
A series of caudatin derivatives were synthesized, and their anti-hepatitis B virus (HBV) activity was evaluated in HepG 2.2.15 cells. Most of the 3-O-substituted caudatin derivatives showed effective anti-HBV activity. Among the tested compounds, six compounds (2e-2h, 2l, 2r) exhibited significantly inhibitory activity against HBV DNA replication with IC50 values in the range of 2.82-7.48 渭M. Interestingly, two compounds (2e, 2f) had potent activity inhibiting not only the secretion of HBsAg (IC50 = 18.68 渭M, 21.71 渭M), HBeAg (IC50 = 13.16 渭M, 33.73 渭M), but also HBV DNA replication (IC50 = 7.48 渭M, 3.63 渭M). The structure-activity relationships (SARs) of caudatin derivatives had been discussed, which were useful for caudatin derivatives to be explored and developed as novel anti-HBV agents.