2. Academic Validation
  3. Discovery and structure activity relationship of glyoxamide derivatives as anti-hepatitis B virus agents

Discovery and structure activity relationship of glyoxamide derivatives as anti-hepatitis B virus agents

  • Bioorg Med Chem. 2021 Feb 1:31:115952. doi: 10.1016/j.bmc.2020.115952.
Franck Amblard 1,  Sebastien Boucle 1,  Leda Bassit 1,  Zhe Chen 1,  Ozkan Sari 1,  Bryan Cox 1,  Kiran Verma 1,  Tugba Ozturk 1,  Olivia Ollinger-Russell 1,  Raymond F Schinazi 2
Affiliations

Affiliations

  • 1 Center for AIDS Research, Laboratory of Biochemical Pharmacology, Department of Pediatrics, Emory University School of Medicine and Children's Healthcare of Atlanta, Atlanta, GA 30322, USA.
  • 2 Center for AIDS Research, Laboratory of Biochemical Pharmacology, Department of Pediatrics, Emory University School of Medicine and Children's Healthcare of Atlanta, Atlanta, GA 30322, USA. Electronic address: rschina@emory.edu.
PMID: 33421915 DOI: 10.1016/j.bmc.2020.115952
Abstract

Chronic hepatitis B viral Infection is a significant health problem world-wide, and currently available Antiviral agents suppress HBV infections, but rarely cure this disease. It is presumed that Antiviral agents that target the viral nuclear reservoir of transcriptionally active cccDNA may eliminate HBV Infection. Through a series of chemical optimization, we identified a new series of glyoxamide derivatives affecting HBV nucleocapsid formation and cccDNA maintenance at low nanomolar levels. Among all the compounds synthesized, GLP-26 displays a major effect on HBV DNA, HBeAg secretion and cccDNA amplification. In addition, GLP-26 shows a promising pre-clinical profile and long-term effect on viral loads in a humanized mouse model.

Keywords

Antiviral; Capsid; Hepatitis B virus; cccDNA.

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