Syntheses and anti-inflammatory activity of azamollugin derivatives

Bioorg Med Chem Lett. 2016 Jan 15;26(2):524-525. doi: 10.1016/j.bmcl.2015.11.081. Epub 2015 Nov 24.

Abstract

Oxomollugin (2) is a degradation product of mollugin (1) and a potent inhibitor of NO-production including nuclear factor kappa B signals. In our endeavor to develop a potent anti-inflammatory compound, we synthesized several aza-derivatives of oxomollugin (2) and evaluated their NO-production inhibitory activity. Azamollugin (3) showed a potent inhibitory activity, and its activity (IC50 0.34μM) was proved to be more potent than that of oxomollugin (2, IC50 1.3μM).

Keywords: Anti-inflammation; Azamollugin; Mollugin; NO-production inhibitor; Oxomollugin.

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*
  • Benzopyrans / chemical synthesis
  • Benzopyrans / pharmacology
  • Cell Line
  • Lipopolysaccharides / pharmacology
  • Mice
  • Nitric Oxide / antagonists & inhibitors*
  • Quinolones / chemical synthesis
  • Quinolones / pharmacology*

Substances

  • Anti-Inflammatory Agents, Non-Steroidal
  • Benzopyrans
  • Lipopolysaccharides
  • Quinolones
  • azamollugin
  • oxomollugin
  • Nitric Oxide