Chemical modification of coumarin dimer and HIV-1 integrase inhibitory activity

Chem Pharm Bull (Tokyo). 2002 Dec;50(12):1634-7. doi: 10.1248/cpb.50.1634.

Abstract

A systematic series of chemically modified coumarin dimmers has been synthesized and tested for their inhibitory activity against HIV-1 integrase. We observed that modified coumarin dimmers containing hydrophobic moiety on the linker display potent inhibitory activities.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Coumarins / chemical synthesis*
  • Coumarins / chemistry
  • Coumarins / pharmacology*
  • Dimerization
  • HIV Integrase / metabolism
  • HIV Integrase Inhibitors / chemical synthesis*
  • HIV Integrase Inhibitors / chemistry
  • HIV Integrase Inhibitors / pharmacology*
  • HIV-1 / drug effects
  • HIV-1 / enzymology*
  • Humans
  • Magnetic Resonance Spectroscopy
  • Molecular Structure
  • Structure-Activity Relationship

Substances

  • Coumarins
  • HIV Integrase Inhibitors
  • HIV Integrase