Oxadiazepinone HBV capsid assembly modulators

Bioorg Med Chem Lett. 2021 Nov 15:52:128353. doi: 10.1016/j.bmcl.2021.128353. Epub 2021 Sep 4.

Abstract

The HBV core protein serves multiple essential functions in the viral life cycle that enable chronic HBV infection to persist, and as such, represents a promising drug target. Modulation of the HBV capsid assembly has shown efficacy in early clinical trials through use of small molecule capsid assembly modulators (CAMs). Herein is described the evolution and SAR of a novel pyrazolo piperidine lead series into advanced oxadiazepinone HBV CAMs.

MeSH terms

  • Antiviral Agents / chemistry
  • Antiviral Agents / pharmacology*
  • Azepines / chemistry
  • Azepines / pharmacology*
  • Capsid Proteins / antagonists & inhibitors*
  • Capsid Proteins / metabolism
  • Dose-Response Relationship, Drug
  • Hepatitis B virus / drug effects*
  • Hepatitis B virus / metabolism
  • Humans
  • Microbial Sensitivity Tests
  • Molecular Structure
  • Structure-Activity Relationship

Substances

  • Antiviral Agents
  • Azepines
  • Capsid Proteins