Synthesis and Anti-Hepatitis B Virus Evaluation of 7-Methoxy-3-heterocyclic quinolin-6-ols.

: A series of novel 7-methoxy-3-heterocyclic quinolin-6-ol derivatives were synthesized and evaluated for their anti-hepatitis B virus (HBV) activities and cytotoxicities in the HepG2.2.15 cell line. Five compounds, 14a, 15c, 15e, 16b, and 16f, displayed excellent potency and selectivity toward the HBV, with IC50 values of less than 5.0 µM and selectivity index values of 11.0-71.5. Structure-activity relationship studies indicated that the 1,3,4-thiadiazole and sulfinylmethyl derivatives showed the most potent activities against the HBV.