title: Syntheses and anti-inflammatory activity of azamollugin derivatives.
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).
authors.affiliation: Faculty of Pharmaceutical Sciences, Hoshi University, Ebara 2-4-41, Shinagawa-ku, Tokyo 142-8501, Japan.
authors.forename: Hitomi
authors.initials: H
authors.lastname: Nishino
authors.affiliation: Faculty of Pharmaceutical Sciences, Hoshi University, Ebara 2-4-41, Shinagawa-ku, Tokyo 142-8501, Japan.
authors.forename: Yuki
authors.initials: Y
authors.lastname: Nakajima
authors.affiliation: Faculty of Pharmaceutical Sciences, Hoshi University, Ebara 2-4-41, Shinagawa-ku, Tokyo 142-8501, Japan.
authors.forename: Yoshiaki
authors.initials: Y
authors.lastname: Kakubari
authors.affiliation: Faculty of Pharmaceutical Sciences, Hoshi University, Ebara 2-4-41, Shinagawa-ku, Tokyo 142-8501, Japan.
authors.forename: Nakata
authors.initials: N
authors.lastname: Asami
authors.affiliation: Faculty of Pharmaceutical Sciences, Hoshi University, Ebara 2-4-41, Shinagawa-ku, Tokyo 142-8501, Japan.
authors.forename: Jun
authors.initials: J
authors.lastname: Deguchi
authors.affiliation: Faculty of Pharmaceutical Sciences, Hoshi University, Ebara 2-4-41, Shinagawa-ku, Tokyo 142-8501, Japan.
authors.forename: Alfarius Eko
authors.initials: AE
authors.lastname: Nugroho
authors.affiliation: Faculty of Pharmaceutical Sciences, Hoshi University, Ebara 2-4-41, Shinagawa-ku, Tokyo 142-8501, Japan.
authors.forename: Yusuke
authors.initials: Y
authors.lastname: Hirasawa
authors.affiliation: Faculty of Pharmaceutical Sciences, Hoshi University, Ebara 2-4-41, Shinagawa-ku, Tokyo 142-8501, Japan.
authors.forename: Toshio
authors.initials: T
authors.lastname: Kaneda
authors.affiliation: National Institute of Health Sciences, 1-18-1 Kamiyoga, Setagaya-ku, Tokyo 158-8501, Japan.
authors.forename: Yoko
authors.initials: Y
authors.lastname: Kawasaki
authors.affiliation: National Institute of Health Sciences, 1-18-1 Kamiyoga, Setagaya-ku, Tokyo 158-8501, Japan.
authors.forename: Yukihiro
authors.initials: Y
authors.lastname: Goda
authors.affiliation: Faculty of Pharmaceutical Sciences, Hoshi University, Ebara 2-4-41, Shinagawa-ku, Tokyo 142-8501, Japan. Electronic address: moritah@hoshi.ac.jp.
authors.forename: Hiroshi
authors.initials: H
authors.lastname: Morita
mesh_terms: D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000138:chemical synthesis / Q000494:pharmacology*; D001578:Benzopyrans / Q000138:chemical synthesis / Q000494:pharmacology; D002460:Cell Line; D008070:Lipopolysaccharides / Q000494:pharmacology; D051379:Mice; D009569:Nitric Oxide / Q000037:antagonists & inhibitors*; D015363:Quinolones / Q000138:chemical synthesis / Q000494:pharmacology*
chemical_list: D000894:Anti-Inflammatory Agents, Non-Steroidal; D001578:Benzopyrans; D008070:Lipopolysaccharides; D015363:Quinolones; C000613477:azamollugin; C000613478:oxomollugin; D009569:Nitric Oxide
keywords: Anti-inflammation; Azamollugin; Mollugin; NO-production inhibitor; Oxomollugin