Preparation and antitussive, expectorant, and antiasthmatic activities of verticinone's derivatives.
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.
Zhang
Yong-Hui
YH
Faculty of Pharmaceutical Sciences, Tongji Medical College, Huazhong University of Science and Technology, Wuhan, China.
Ruan
Han-Li
HL
Pi
Hui-Fang
HF
Wu
Ji-Zhou
JZ
Sun
Han-Dong
HD
Fujita
Tetsuro
T
D000818:Animals; D000996:Antitussive Agents / Q000737:chemistry* / Q000494:pharmacology; D001249:Asthma / Q000188:drug therapy; D001993:Bronchodilator Agents / Q000737:chemistry* / Q000494:pharmacology; D002595:Cevanes / Q000737:chemistry*; D003371:Cough / Q000188:drug therapy; D005100:Expectorants / Q000737:chemistry* / Q000494:pharmacology; D005260:Female; D006168:Guinea Pigs; D008297:Male; D051379:Mice; D015394:Molecular Structure; D013329:Structure-Activity Relationship
D000996:Antitussive Agents; D001993:Bronchodilator Agents; D002595:Cevanes; D005100:Expectorants; C014242:verticine