Synthesis and HIV-1 integrase inhibitory activities of caffeic acid dimers derived from Salvia officinalis.

Abstract

The synthesis of two caffeoyl-coumarin conjugates, derived from sagecoumarin, has been accomplished, starting from ferulic acid, isoferulic acid and sesamol. Both compounds exhibited potent inhibitory activities at micromolar concentrations against HIV-1 integrase in 3'-end processing reaction but were less effective against HIV-1 replication in a single-round infection assay of HeLa-beta-gal-CD4+ cells.

• Authors: Fabrice Bailly, Clémence Queffelec, Gladys Mbemba, Jean-François Mouscadet, Philippe Cotelle
• Journal: Bioorganic & medicinal chemistry letters (Bioorg Med Chem Lett) Vol. 15 Issue 22 Pg. 5053-6 (Nov 15 2005) ISSN: 0960-894X [Print] England
• PMID: 16183277 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Caffeic Acids
• Coumarins
• HIV Integrase Inhibitors
• coumarin
• HIV Integrase

Topics

• Caffeic Acids (chemical synthesis, chemistry, isolation & purification, pharmacology)
• Coumarins (chemistry)
• Dimerization
• HIV Integrase (metabolism)
• HIV Integrase Inhibitors (chemical synthesis, chemistry, isolation & purification, pharmacology)
• Inhibitory Concentration 50
• Molecular Structure
• Salvia officinalis (chemistry)