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
  • 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: [email protected].
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.