The octadecyloxyethyl ester of (S)-9-[3-hydroxy-2-(phosphonomethoxy) propyl]adenine is a potent and selective inhibitor of hepatitis C virus replication in genotype 1A, 1B, and 2A replicons

Antimicrob Agents Chemother. 2009 Jun;53(6):2660-2. doi: 10.1128/AAC.01546-08. Epub 2009 Mar 16.

Abstract

The octadecyloxyethyl (ODE) and hexadecyloxypropyl (HDP) esters of (S)-9-[3-hydroxy-2-(phosphonomethoxy)propyl]adenine (HPMPA) are potent inhibitors of orthopoxvirus, herpesvirus, human immunodeficiency virus type 1, and hepatitis B virus replication in vitro. HDP and ODE esters of (S)-HPMPA and (R)-HPMPA were evaluated for their activity in hepatitis C virus (HCV) replicon assays using luciferase (1B and 2A replicons) or RNA (1B) quantification. The ODE ester of (S)-HPMPA [ODE-(S)-HPMPA] was the most active compound, with 50% effective concentrations (EC(50)s) in the 0.69 to 1.31 microM range. HDP and ODE esters of (R)-HPMPA were severalfold less active, while (S)-HPMPA and (R)-HPMPA were inactive. In genotype 1A and 1B replicons analyzed by HCV RNA analysis, ODE-(S)-HPMPA was the most active compound, with EC(50)s of 1.8 and 2.1 microM, respectively.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Adenine / analogs & derivatives*
  • Adenine / pharmacology
  • Antiviral Agents / pharmacology*
  • Esters / pharmacology
  • Genotype
  • Hepacivirus / classification
  • Hepacivirus / drug effects*
  • Hepacivirus / genetics
  • Organophosphonates / pharmacology*
  • Plasmids
  • Replicon*
  • Structure-Activity Relationship
  • Virus Replication / drug effects*

Substances

  • Antiviral Agents
  • Esters
  • Organophosphonates
  • 9-(S)-(3-hydroxy-2-(phosphonomethoxy)propyl)adenine
  • Adenine