Synthesis and anti-HBV activities evaluation of new ethyl 8-imidazolylmethyl-7-hydroxyquinoline-3-carboxylate derivatives in vitro

Some new ethyl 8-imidazolylmethyl-7-hydroxyquinoline-3-carboxylate derivatives have been synthesized and evaluated for their anti-hepatitis B virus (HBV) activities and cytotoxicities in HepG2.2.15 cells stable transfection with HBV. Compounds 13a, 11b, 11c, 12c, 13c, 11g, and 12g inhibited the expression of the viral antigens HBsAg or HBeAg in a low concentration, of which 11c (IC50 = 12.6 mu M, SI = 12.4), 12c (IC50 = 3.5 mu M, SI = 37.9), and 12g (IC50 = 2.6 mu M, SI = 61.6) showed more active abilities to inhibit the replication of HBV DNA than the positive control lamivudine (3TC, IC50 = 343.2 mu M, SI = 7.0).