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Preparation and antitussive, expectorant, and antiasthmatic activities of verticinone's derivatives

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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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Keywords: 3-acetylverticinone derivative; antiasthmatic; antitussive; expectorant; verticinone

Document Type: Research Article

Affiliations: 1: Faculty of Pharmaceutical Sciences, Tongji Medical College, Huazhong University of Science and Technology, Wuhan, China 2: Kunming Institute of Botany, Chinese Academy of Sciences, Kunming, China 3: Faculty of Pharmaceutical Sciences, Kyoto University, Kyoto, Japan

Publication date: July 1, 2008

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