Design, Synthesis and Bioactive Evaluation of Oxime Derivatives of Dehydrocholic Acid as Anti-Hepatitis B Virus Agents.

ABSTRACT: Oxime derivatives of dehydrocholic acid and its esters were designed for anti-hepatitis B virus (HBV) drugs according to principles of assembling active chemical fragments. Twelve compounds were synthesized from dehydrocholic acid by esterification and oxime formation, and their anti-hepatitis B virus (HBV) activities were evaluated with HepG 2.2.15 cells. Results showed that 5 compounds exhibited more effective inhibition of HBeAg than positive control, among them 2b-3 and 2b-1 showed significant anti-HBV activities on inhibiting secretion of HBeAg (IC_{50 (2b-3)} = 49.39 ± 12.78 μM, SI _(2b-3) = 11.03; IC_{50 (2b-1)} = 96.64 ± 28.99 μM, SI _(2b-1) = 10.35) compared to the Entecavir (IC₅₀ = 161.24 μM,

SUBMITTER: Wei Z 

PROVIDER: S-EPMC7435646 | biostudies-literature | 2020 Jul

REPOSITORIES: biostudies-literature