Abstract
Small molecule induced hepatitis B virus (HBV) capsid assembly modulation is considered an attractive approach for new antiviral therapies against HBV. Here we describe efforts toward the discovery of a HBV capsid assembly modulator in a hit-to-lead optimization, resulting in JNJ-632, a tool compound used to further profile the mode of action. Administration of JNJ-632 (54) in HBV genotype D infected chimeric mice resulted in a 2.77 log reduction of the HBV DNA viral load.
MeSH terms
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Animals
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Antiviral Agents / chemical synthesis*
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Antiviral Agents / chemistry
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Antiviral Agents / metabolism
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Antiviral Agents / pharmacology*
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Benzamides / chemical synthesis*
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Benzamides / chemistry
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Benzamides / metabolism
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Benzamides / pharmacology*
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Capsid / drug effects*
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Capsid / metabolism
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Chemistry Techniques, Synthetic
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Genotype
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Hepatitis B virus / drug effects*
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Hepatitis B virus / genetics
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Hepatitis B virus / metabolism*
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Hepatitis B virus / physiology
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Humans
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Mice
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Molecular Docking Simulation
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Protein Conformation
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Sulfonamides / chemical synthesis*
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Sulfonamides / chemistry
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Sulfonamides / metabolism
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Sulfonamides / pharmacology*
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Viral Load / drug effects
Substances
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Antiviral Agents
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Benzamides
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JNJ-632
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Sulfonamides