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

Abstract

To prepare verticinone derivatives with significant antitussive, expectorant, and antiasthmatic activities, the compounds 3β-acetylverticinone (1), 3-ketoverticinone (2), 3β-benzoylverticinone (3), 3β-propionylverticinone (4), 3β-butyrylverticinone (5), and 3β-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.

Keywords:

• verticinone
• 3β-acetylverticinone derivative
• antitussive
• expectorant
• antiasthmatic

Acknowledgements

The authors are grateful for the financial support from the National Natural Science Foundation of China (NSFC, no. 30572313) and the Great foundation on Society Development of China, Hubei provincial Science & Technology Department (no. 2003AA302B08).