Synthesis and evaluation of 3'-azido-2',3'-dideoxypurine nucleosides as inhibitors of human immunodeficiency virus

  • Bioorg Med Chem Lett. 2010 Jan 1;20(1):60-4. doi: 10.1016/j.bmcl.2009.11.031.
Hong-Wang Zhang  1 ,  Steven J Coats ,  Lavanya Bondada ,  Franck Amblard ,  Mervi Detorio ,  Ghazia Asif ,  Emilie Fromentin ,  Sarah Solomon ,  Aleksandr Obikhod ,  Tony Whitaker ,  Nicolas Sluis-Cremer ,  John W Mellors ,  Raymond F Schinazi
Affiliations
  • 1. Center for AIDS Research, Laboratory of Biochemical Pharmacology, Department of Pediatrics, Emory University School of Medicine, and Veterans Affairs Medical Center, Atlanta, GA 30033, USA.
PMID: 19948402 DOI: 10.1016/j.bmcl.2009.11.031
Abstract

Based on the promising drug resistance profile and potent anti-HIV activity of beta-d-3'-azido-2',3'-dideoxyguanosine, a series of purine modified nucleosides were synthesized by a chemical transglycosylation reaction and evaluated for their Antiviral activity, cytotoxicity, and intracellular metabolism. Among the synthesized compounds, several show potent and selective anti-HIV activity in primary lymphocytes.