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. 2023 Aug 15:92:129350.
doi: 10.1016/j.bmcl.2023.129350. Epub 2023 May 27.

Di-fluoro azepane HBV capsid assembly modulators

Lindsey G DeRatt  1 , Bart Stoops  2 , Paul Shaffer  3 , Angela M Lam  3 , Christine Espiritu  3 , Robert Vogel  3 , Vincent Lau  3 , Osvaldo A Flores  3 , Scott D Kuduk  4
Affiliations

Di-fluoro azepane HBV capsid assembly modulators

Lindsey G DeRatt et al. Bioorg Med Chem Lett. .

Abstract

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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Conflict of interest statement

Declaration of Competing Interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.

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