Bioorganic & Medicinal Chemistry Letters 2016-01-15

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

文献索引：Bioorg. Med. Chem. Lett. 26(2) , 524-5, (2016)

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摘要

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.