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 3beta-acetylverticinone (1), 3-ketoverticinone (2), 3beta-benzoylverticinone (3), 3beta-propionylverticinone (4), 3beta-butyrylverticinone (5), and 3beta-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.

Synthesis of peiminine derivatives and its effect on A549 lung cancer‐bearing mice

“…Therefore, it is necessary to modify peiminine in order to obtain derivatives with improved solubility and higher pharmacological activity. Zhang Yonnghui et al (Zhang et al., 2008) found that the verticinone derivative 3‐acetylverticinone has higher anti‐asthmatic activity than verticinone. This indicts that the 3‐OH (C‐3) may represent the active site of peiminine.…”