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

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Abstract:

With the aim of obtaining potential IL-6 inhibitor for the treatment of rheumatoid arthritis, four 3-aryloxylindolizine derivatives were synthesized from the 2-bromopyridine 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 μM. The bioactive 3-aryloxylindolizines might be used as potential anti-inflammatory drugs.

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Advanced Materials Research (Volumes 781-784)

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1093-1097

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September 2013

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© 2013 Trans Tech Publications Ltd. All Rights Reserved

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