Synthesis and Anti-inflammatory Activity of 3-Aryloxylindolizine Derivatives via Sonogashira Coupling! 5-endo-trig Cycloisomerization Domino Strategy

摘要

With the aim of obtaining potential IL-6 inhibitor for the treatment of rheumatoid arthritis, four 3-aryloxylindolizine derivatives were synthesized from the 2-bromopyridinc and aryl propargyl ether through the Sonogashira coupling/5-endo-trig cycloisomerization domino strategy. These compounds were characterized by NMR, IR, EI-MS and elemental analysis. Their biological activities were evaluated by the bacterial lipopolysaccharide (LPS) stimulation of mouse cells on the RAW264.7 inflammation model. All the compounds revealed good anti-inflammatory activities with the inhibitions of 71-82% against IL-6 at 100 |iM. The bioactivc 3-aryloxylindolizines might be used as potential anti-inflammatory drugs.