To prepare verticinone derivatives with significant antitussive, expectorant, and antiasthmatic activities, the compounds 3-acetylverticinone (1), 3-ketoverticinone (2), 3-benzoylverticinone (3), 3-propionylverticinone (4), 3-butyrylverticinone (5), and 3-butoxycarbonylverticinone (6) have been prepared. All of these are new compounds. Among them, 1-6 exhibited potent antitussive and expectorant activities; 1 and 3-6 displayed various antiasthmatic activities. The antitussive activity of 1-6, the expectorant activity of 1-2 and 4-6, and the antiasthmatic activity of 1 are higher than those of verticinone. The results demonstrated that 1 had dominant biological activities, suggesting that it would be a potential antitussive, expectorant, and antiasthmatic agent.
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Document Type: Research Article
Faculty of Pharmaceutical Sciences, Tongji Medical College, Huazhong University of Science and Technology, Wuhan, China
Kunming Institute of Botany, Chinese Academy of Sciences, Kunming, China
Faculty of Pharmaceutical Sciences, Kyoto University, Kyoto, Japan
July 1, 2008