Syntheses and anti-inflammatory activity of azamollugin derivatives.
Hitomi Nishino, Yuki Nakajima, Yoshiaki Kakubari, Nakata Asami, Jun Deguchi, Alfarius Eko Nugroho, Yusuke Hirasawa, Toshio Kaneda, Yoko Kawasaki, Yukihiro Goda, Hiroshi Morita
Index: Bioorg. Med. Chem. Lett. 26(2) , 524-5, (2016)
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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).Copyright © 2015 Elsevier Ltd. All rights reserved.
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