1. Academic Validation
  2. Synthesis and antiviral evaluation of 2-amino-6-carbamoylpurine dioxolane nucleoside derivatives and their phosphoramidates prodrugs

Synthesis and antiviral evaluation of 2-amino-6-carbamoylpurine dioxolane nucleoside derivatives and their phosphoramidates prodrugs

  • Bioorg Med Chem. 2014 Dec 1;22(23):6665-6671. doi: 10.1016/j.bmc.2014.10.003.
Jong Hyun Cho 1 Lavanya Bondana 1 Mervi A Detorio 1 Cathy Montero 1 Leda C Bassit 1 Franck Amblard 1 Steven J Coats 2 Raymond F Schinazi 1
Affiliations

Affiliations

  • 1 Center for AIDS Research, Laboratory of Biochemical Pharmacology, Department of Pediatrics, Emory University School of Medicine, and Veterans Affairs Medical Center, 1670 Haygood Drive, NE, Atlanta, GA 30322, USA.
  • 2 RFS Pharma, LLC, 1860 Montreal Road, Tucker, GA 30084, USA.
Abstract

The synthesis of 9-(β-d-1,3-dioxolan-4-yl)2,6-diaminopurine nucleoside phosphoramidate prodrugs as well as various 2-amino-6-carbamoylpurine dioxolane derivatives and their phosphoramidates prodrugs is reported. Their ability to block HIV and HBV replication along with their cytotoxicity toward HepG2, human lymphocyte, CEM and Vero cells was also assessed.

Keywords

Anti-HBV; Anti-HIV; Antiviral agent; DAPD; β-d-1,3-Dioxolan-4-yl nucleosides.

Figures