Antiviral Evaluation of Dispirotripiperazines against Hepatitis B Virus.

ABSTRACT: Hepatitis B virus (HBV) is a hepatotropic DNA virus that replicates by reverse transcription. It chronically infects >296 million people worldwide, including ∼850,000 in the USA, and kills 820,000 annually worldwide. Current nucleos(t)ide analogue (NA) or pegylated interferon α therapies do not eradicate the virus and would benefit from a complementary antiviral drug. We performed a preliminary screen of 28 dispirotripiperazines against HBV, identifying 9 hits with EC₅₀ of 0.7-25 μM. Compound 11826096 displays the most potent activity and represents a promising lead for future optimization. While the mechanism of action is unknown, preliminary assays limit possible targets to activities involved in RNA accumulation, translation, capsid assembly, and/or capsid stability. In addit

SUBMITTER: Jones T 

PROVIDER: S-EPMC11017374 | biostudies-literature | 2023 Sep

REPOSITORIES: biostudies-literature