Simple aromatic compounds containing propenone moiety show considerable dual COX/5-LOX inhibitory activities

Bioorg Med Chem Lett. 2004 May 17;14(10):2559-62. doi: 10.1016/j.bmcl.2004.02.099.

Abstract

For the development of safer anti-inflammatory agents, simple aromatic compounds containing propenone moiety were prepared and evaluated for their dual COX/5-LOX inhibitory activities. Among the 17 prepared compounds, most of the compounds exhibited considerable COX/5-LOX inhibitory activities. Especially compound C(15) showed the most significant dual COX/5-LOX inhibitory activity.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Anti-Inflammatory Agents, Non-Steroidal / chemical synthesis*
  • Anti-Inflammatory Agents, Non-Steroidal / pharmacology
  • Bone Marrow Cells / enzymology
  • Cyclooxygenase Inhibitors / chemical synthesis*
  • Cyclooxygenase Inhibitors / pharmacology
  • Drug Design
  • Enzyme Inhibitors / chemical synthesis
  • Enzyme Inhibitors / pharmacology
  • Hydrocarbons, Aromatic / chemical synthesis
  • Hydrocarbons, Aromatic / pharmacology*
  • Inhibitory Concentration 50
  • Ketones / chemical synthesis
  • Ketones / pharmacology
  • Lipoxygenase Inhibitors*
  • Male
  • Mice
  • Mice, Inbred BALB C
  • Structure-Activity Relationship

Substances

  • Anti-Inflammatory Agents, Non-Steroidal
  • Cyclooxygenase Inhibitors
  • Enzyme Inhibitors
  • Hydrocarbons, Aromatic
  • Ketones
  • Lipoxygenase Inhibitors