Syntheses and anti-inflammatory activity of azamollugin derivatives. Issue 2 (15th January 2016)

• Record Type: Journal Article
• Authors: Nishino, Hitomi; Nakajima, Yuki; Kakubari, Yoshiaki; Asami, Nakata; Deguchi, Jun; Nugroho, Alfarius Eko; Hirasawa, Yusuke; Kaneda, Toshio; Kawasaki, Yoko; Goda, Yukihiro; Morita, Hiroshi
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 26:Issue 2(2016)
• Page Start: 524
• Page End: 525
• Publication Date: 2016-01-15
• Subjects: Azamollugin -- Oxomollugin -- Mollugin -- Anti-inflammation -- NO-production inhibitor; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2015.11.081
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: 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 0.34 μM) was proved to be more potent than that of oxomollugin (2, IC50 1.3 μM).