Synthesis and Evaluation of N‑Phenyl-3-sulfamoyl-benzamide Derivatives as Capsid Assembly Modulators Inhibiting Hepatitis B Virus (HBV)

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 compoun...

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Veröffentlicht in:Journal of medicinal chemistry 2018-07, Vol.61 (14), p.6247-6260
Hauptverfasser: Vandyck, Koen, Rombouts, Geert, Stoops, Bart, Tahri, Abdellah, Vos, Ann, Verschueren, Wim, Wu, Yiming, Yang, Jingmei, Hou, Fuliang, Huang, Bing, Vergauwen, Karen, Dehertogh, Pascale, Berke, Jan Martin, Raboisson, Pierre
Format: Artikel
Sprache:eng
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Zusammenfassung: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.
ISSN:0022-2623
1520-4804
DOI:10.1021/acs.jmedchem.8b00654