4.5 Article

Di-fluoro azepane HBV capsid assembly modulators

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 92, Issue -, Pages -

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2023.129350

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The capsid core protein of the HBV virus is essential for the persistence of chronic HBV infections. Disrupting the assembly of the capsid has shown promise in combating the virus, and a new series of di-fluoro azepane CAMs with exceptional properties has been described in this study.
The protein that forms the inner shell of the HBV virus, known as the capsid core protein, plays a crucial role in allowing chronic HBV infections to persist. Studies have shown that disrupting the assembly of the capsid can effectively combat the virus, and small molecule drugs that target the HBV capsid assembly modulator (CAM) process have been successful in clinical trials. Herein is described a distinct series of di-fluoro azepane CAMs with exceptional potency, pharmacokinetic, and solubility properties.

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