Comparative activity of various compounds against clinical strains of herpes simplex virus

Eur J Clin Microbiol Infect Dis. 1992 Feb;11(2):143-51. doi: 10.1007/BF01967066.

Abstract

The following compounds were evaluated for their inhibitory activity against clinical strains of herpes simplex virus type 1 (HSV-1) and type 2 (HSV-2) in both primary rabbit kidney (PRK) and HeLa cell cultures: (S)-9-(3-hydroxy-2-phosphonylmethoxypropyl)adenine (HPMPA), 9-(2-phosphonylmethoxyethyl)adenine (PMEA), (S)-1-(3-hydroxy-2-phosphonylmethoxypropyl)cytosine (HPMPC), (RS)-9-(3-hydroxy-2-phosphonylmethoxypropyl)-2,6-diaminopurine (HPMPDAP), 5-(5-bromothien-2-yl)-2'-deoxyuridine (BTDU), 5-(5-chlorothien-2-yl)-2'-deoxyuridine (CTDU), 9-(2-deoxy-2-hydroxymethyl-beta-D-erythro-oxetanosyl)guanine (OXT-G), pentosan polysulfate, heparin, dextran sulfate (MW 10,000), acyclovir, 9-(2-hydroxyethoxymethyl)guanine (ACV), (E)-5-(2-bromovinyl)-2'-deoxyuridine (BVDU), 1-beta-D-arabinofuranosyl-(E)-5-(2-bromovinyl)-uracil (BVaraU), vidarabine (9-beta-D-arabinofuranosyladenine) (ara-A) and phosphonoformate (PFA). The most potent inhibitors of HSV-1 were (in order of decreasing activity in PRK cells) BVDU, ACV, BVaraU and OXT-G, their mean 50% inhibitory concentration (IC50) ranging from 0.02 micrograms/ml to 0.9 micrograms/ml. Then followed BTDU and CTDU (IC50 1-2 micrograms/ml), the sulfated polysaccharides (IC50 1.3-5.8 micrograms/ml), the phosphonylmethoxyalkyl derivatives (IC50 5.6-25 micrograms/ml),ara-A (IC50 11 micrograms/ml) and PFA (IC50 38.5 micrograms/ml). Except for BVDU, BVaraU, BTDU and CTDU, the compounds did not discriminate between HSV-2 and HSV-1. All the compounds studied could be considered specific anti-HSV agents. Their selectivity indexes varied from 3 (PFA) to 6400 (BVDU).

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acyclovir / pharmacology
  • Adenine / analogs & derivatives
  • Adenine / pharmacology
  • Animals
  • Antiviral Agents / pharmacology*
  • Cidofovir
  • Cytopathogenic Effect, Viral / drug effects
  • Cytosine / analogs & derivatives
  • Cytosine / pharmacology
  • Dextran Sulfate / pharmacology
  • Guanine / analogs & derivatives
  • Guanine / pharmacology
  • HeLa Cells
  • Heparin / pharmacology
  • Humans
  • Nucleosides / pharmacology
  • Organophosphonates*
  • Organophosphorus Compounds / pharmacology
  • Rabbits
  • Simplexvirus / drug effects*
  • Simplexvirus / physiology
  • Virus Replication / drug effects

Substances

  • Antiviral Agents
  • Nucleosides
  • Organophosphonates
  • Organophosphorus Compounds
  • oxetanocin G
  • 9-(3-hydroxy-2-phosphonomethoxypropyl)-2,6-diaminopurine
  • Guanine
  • Cytosine
  • Heparin
  • Dextran Sulfate
  • Adenine
  • Cidofovir
  • Acyclovir