Design and synthesis of benzo-lipoxin A4 analogs with enhanced stability and potent anti-inflammatory properties

Bioorg Med Chem Lett. 2008 Feb 15;18(4):1382-7. doi: 10.1016/j.bmcl.2008.01.013. Epub 2008 Jan 9.

Abstract

A new class of chemically and metabolically stable lipoxin analogs featuring a replacement of the tetraene unit of native LXA(4) with a substituted benzo-fused ring system have been designed and studied. These molecules were readily synthesized via a convergent synthetic route involving iterative palladium-mediated cross-coupling, and exhibit enhanced chemical stability, as well as resistance to metabolic inactivation via eicosanoid oxido-reductase. These new LX analogs were evaluated in a model of acute inflammation and were shown to exhibit potent anti-inflammatory properties, significantly decreasing neutrophil infiltration in vivo. The most potent among these was compound 9 (o-[9,12]-benzo-15-epi-LXA(4) methyl ester. Taken together, these findings help identify a new class of stable and easily prepared LX analogs that may serve as novel tools and as promising leads for new anti-inflammatory agents with improved therapeutic profile.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Animals
  • Anti-Inflammatory Agents, Non-Steroidal / chemical synthesis*
  • Anti-Inflammatory Agents, Non-Steroidal / chemistry
  • Anti-Inflammatory Agents, Non-Steroidal / pharmacology*
  • Benzene Derivatives / chemical synthesis*
  • Benzene Derivatives / pharmacology*
  • Drug Design
  • Drug Stability
  • Lipoxins / chemical synthesis*
  • Lipoxins / chemistry
  • Lipoxins / metabolism
  • Lipoxins / pharmacology*
  • Mice
  • Neutrophil Infiltration / drug effects
  • Oxidoreductases / chemistry
  • Oxidoreductases / metabolism
  • Peritonitis / drug therapy

Substances

  • Anti-Inflammatory Agents, Non-Steroidal
  • Benzene Derivatives
  • Lipoxins
  • lipoxin A4
  • Oxidoreductases