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.
Hitomi Nishino  1 ,  Yuki Nakajima  1 ,  Yoshiaki Kakubari  1 ,  Nakata Asami  1 ,  Jun Deguchi  1 ,  Alfarius Eko Nugroho  1 ,  Yusuke Hirasawa  1 ,  Toshio Kaneda  1 ,  Yoko Kawasaki  2 ,  Yukihiro Goda  2 ,  Hiroshi Morita  3
Affiliations
  • 1. Faculty of Pharmaceutical Sciences, Hoshi University, Ebara 2-4-41, Shinagawa-ku, Tokyo 142-8501, Japan.
  • 2. National Institute of Health Sciences, 1-18-1 Kamiyoga, Setagaya-ku, Tokyo 158-8501, Japan.
  • 3. Faculty of Pharmaceutical Sciences, Hoshi University, Ebara 2-4-41, Shinagawa-ku, Tokyo 142-8501, Japan. Electronic address: [email protected].
PMID: 26681510 DOI: 10.1016/j.bmcl.2015.11.081
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.