Abstract
The HBV core protein is a druggable target of interest due to the multiple essential functions in the HBV life cycle to enable chronic HBV infection. The core protein oligomerizes to form the viral capsid, and modulation of the HBV capsid assembly has shown efficacy in clinical trials. Herein is described the identification and hit to lead SAR of a novel series of pyrazolo piperidine HBV capsid assembly modulators.
Keywords:
Capsid; HBV; Modulator; Urea.
Copyright © 2021 Elsevier Ltd. All rights reserved.
MeSH terms
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Antiviral Agents / chemistry
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Antiviral Agents / pharmacology*
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Capsid Proteins / antagonists & inhibitors*
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Capsid Proteins / metabolism
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Dose-Response Relationship, Drug
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Hepatitis B virus / drug effects*
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Hepatitis B virus / metabolism
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Microbial Sensitivity Tests
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Molecular Structure
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Piperidines / chemistry
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Piperidines / pharmacology*
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Pyrazoles / chemistry
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Pyrazoles / pharmacology*
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Structure-Activity Relationship
Substances
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Antiviral Agents
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Capsid Proteins
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Piperidines
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Pyrazoles
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pyrazole
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piperidine