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

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

  • J Med Chem. 2018 Jul 26;61(14):6247-6260. doi: 10.1021/acs.jmedchem.8b00654.
Koen Vandyck 1,  Geert Rombouts 1,  Bart Stoops 1,  Abdellah Tahri 1,  Ann Vos 1,  Wim Verschueren 1,  Yiming Wu 2,  Jingmei Yang 2,  Fuliang Hou 2,  Bing Huang 2,  Karen Vergauwen 1,  Pascale Dehertogh 1,  Jan Martin Berke 1,  Pierre Raboisson 1
Affiliations

Affiliations

  • 1 Janssen Pharmaceutica NV , Janssen Pharmaceutical Companies of Johnson & Johnson , Turnhoutseweg 30 , 2340 Beerse , Belgium.
  • 2 WuXi AppTec , 288 Fute Zhong Road , China (Shanghai) Pilot Free Trade Zone; Shanghai 200131 , PR China.
PMID: 29906396 DOI: 10.1021/acs.jmedchem.8b00654
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.

Figures
Products
  • Cat. No.
    Product Name
    Description
    Target
    Research Area
  • HY-112564
    99.61%, HBV 抑制剂
    HBV
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