Synthesis and HIV-1 integrase inhibitory activities of caffeoylglucosides

Bioorg Med Chem Lett. 2000 Aug 21;10(16):1879-82. doi: 10.1016/s0960-894x(00)00355-3.

Abstract

Caffeoylglucosides, which have a glucose ring as a central linker, were synthesized from methyl D-glucosides, and their anti-HIV-1 activities were tested. Among them, four dicaffeoylglucosides (IC50 = 29.1+/-35.1 microM), 6a, 6b, 9b and 10b, showed HIV-1 integrase inhibitory activity as potent as L-chicoric acid.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anti-HIV Agents / chemical synthesis*
  • Anti-HIV Agents / chemistry
  • Anti-HIV Agents / pharmacology
  • Caffeic Acids / chemical synthesis*
  • Caffeic Acids / chemistry
  • Caffeic Acids / pharmacology*
  • Glucosides / chemical synthesis*
  • Glucosides / chemistry
  • Glucosides / pharmacology*
  • HIV Integrase / metabolism*
  • HIV Integrase Inhibitors / chemical synthesis*
  • HIV Integrase Inhibitors / chemistry
  • HIV Integrase Inhibitors / pharmacology*
  • Humans
  • Lamiaceae / chemistry
  • Molecular Structure
  • Plants, Medicinal / chemistry

Substances

  • Anti-HIV Agents
  • Caffeic Acids
  • Glucosides
  • HIV Integrase Inhibitors
  • HIV Integrase