2. Academic Validation
  3. Synthesis and antiviral evaluation of novel heteroarylpyrimidines analogs as HBV capsid effectors

Synthesis and antiviral evaluation of novel heteroarylpyrimidines analogs as HBV capsid effectors

  • Bioorg Med Chem Lett. 2017 Feb 15;27(4):904-910. doi: 10.1016/j.bmcl.2017.01.010.
Sebastien Boucle 1,  Xiao Lu 1,  Leda Bassit 1,  Tugba Ozturk 1,  Olivia Ollinger Russell 1,  Franck Amblard 1,  Steven J Coats 2,  Raymond F Schinazi 3
Affiliations

Affiliations

  • 1 Center for AIDS Research, Laboratory of Biochemical Pharmacology, Department of Pediatrics, Emory University School of Medicine, Atlanta, GA 30322, USA.
  • 2 Cocrystal Pharma, Inc., 1860 Montreal Road, Tucker, GA 30084, USA.
  • 3 Center for AIDS Research, Laboratory of Biochemical Pharmacology, Department of Pediatrics, Emory University School of Medicine, Atlanta, GA 30322, USA. Electronic address: rschina@emory.edu.
PMID: 28094179 DOI: 10.1016/j.bmcl.2017.01.010
Abstract

New modifications to the scaffold of previously reported HBV capsid assembly effectors such as BAY 41-4109, HAP-12 and GLS4 were explored. The anti-HBV activity in the HepAD38 system, and cytotoxicity profiles of each of the new compounds has been assessed. Among them, five new iodo- and bromo-heteroarylpyrimidines analogs displayed anti-HBV activity in the low micromolar range.

Keywords

Capsid assembly effectors; HAP; HBV; Heteroarylpyrimidine.

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