Synthesis and anti-inflammatory activity of natural and semisynthetic geranyloxycoumarins

Bioorg Med Chem Lett. 2004 May 3;14(9):2241-3. doi: 10.1016/j.bmcl.2004.02.009.

Abstract

Nine new 7-geranyloxycoumarin derivatives differently substituted at position 8 were semi-synthesised. Their topical anti-inflammatory activity was evaluated using the Croton oil ear test in mice as a model of acute inflammation. Auraptene (7-geranyloxycoumarin), its 8-methoxy (collinin, 1) and 8-acetoxy derivatives (5) (1 micromol/cm(2)) provoked 50% oedema reduction, similarly to 0.25 micromol/cm(2) of the reference drug indomethacin, a nonsteroidal anti-inflammatory drug.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Anti-Inflammatory Agents / chemical synthesis*
  • Anti-Inflammatory Agents / chemistry
  • Anti-Inflammatory Agents / pharmacology*
  • Coumarins / chemical synthesis*
  • Coumarins / chemistry
  • Coumarins / pharmacology*
  • Male
  • Mice

Substances

  • Anti-Inflammatory Agents
  • Coumarins