Synthesis and anti-hepatitis B virus evaluation of novel ethyl 6-hydroxyquinoline-3-carboxylates in vitro

A series of non-nucleoside ethyl 6-hydroxyquinoline-3-carboxylate derivatives were prepared and evaluated in HepG2.2.15 cells. Most compounds inhibited the expression of viral antigens HBsAg or HBeAg at low concentration. Six compounds, 9f3, 12b6, 12f6, 13b2, 13b6, and 13f6, displayed excellent intracellular inhibitory activity and selectivity towards the replication of HBV DNA. Of these six initial hits, compound 13b6 was the most active.

A series of novel ethyl 6-hydroxyquinoline-3-carboxylates were designed and synthesized, and their inhibitory activities against hepatitis B virus (HBV) were compared to that of lamivudine in HepG2.2.15 cells.Figure optionsDownload as PowerPoint slide