2. Academic Validation
  3. Syntheses and anti-inflammatory activity of azamollugin derivatives

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

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: moritah@hoshi.ac.jp.
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.

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