Chemotherapy of the acquired immune deficiency syndrome (AIDS): non-nucleoside inhibitors of the human immunodeficiency virus type 1 reverse transcriptase

Int J Immunopharmacol. 1991:13 Suppl 1:83-9. doi: 10.1016/0192-0561(91)90129-u.


Several classes of non-nucleotide analogues (i.e. TIBO and HEPT derivatives) have been identified that specifically interact with the reverse transcriptase (RT) of human immunodeficiency virus type 1 (HIV-1). These derivatives inhibit the replication of HIV-1 in various cell lines, including peripheral blood lymphocytes and monocytes/macrophages, at concentrations that are 10,000- to 100,000-fold lower than the cytotoxic concentrations. At the HIV-1 RT level, they appear to interact with a specific allosteric "TIBO" site, which may be functionally and also structurally associated with the substrate binding site. The TIBO and TIBO-like compounds are orally bioavailable. In vivo they sustain plasma drug levels that are well above the concentrations required to inhibit virus replication in vitro.

MeSH terms

  • Acquired Immunodeficiency Syndrome / drug therapy*
  • Antiviral Agents / pharmacology*
  • Antiviral Agents / therapeutic use
  • Benzodiazepines / pharmacology*
  • Benzodiazepines / therapeutic use
  • HIV-1 / drug effects*
  • HIV-1 / enzymology
  • Humans
  • Imidazoles / pharmacology*
  • Imidazoles / therapeutic use
  • Reverse Transcriptase Inhibitors*
  • Thymine / analogs & derivatives*
  • Thymine / pharmacology
  • Thymine / therapeutic use
  • Virus Replication / drug effects


  • Antiviral Agents
  • Imidazoles
  • Reverse Transcriptase Inhibitors
  • 1-((2-hydroxyethoxy)methyl)-6-(phenylthio)thymine
  • Benzodiazepines
  • R-82913
  • Thymine