Digoxin derivatives substituted by alkylidene at the butenolide part

作者：Xu, Hai-Wei; Liu, Gai-Zhi; Zhu, Song-Lin; Hong, Guang-Feng; Liu, Hong-Min^*; Wu, Qiong

来源：Steroids, 2010, 75(6): 419-423.

DOI：10.1016/j.steroids.2010.02.007

• Digoxin
• gamma-Substituted butenolide
• Synthesis
• Myocardial contractility

A series of digoxin derivatives containing the gamma-alkylidene butenolide moiety were synthesised by way of stereoselective vinylogous aldol reaction of the unactivated butenolide in simple conditions. The structures of compounds synthesised were characterised by infrared (IR), nuclear magnetic resonance (NMR) and FIR-MS. Preliminary bioassay shows that some of them have cardiac functions, especially compound 2g that induced a marked increase in myocardial contractility at 10 ng ml(-1) and 20 ng ml(-1) concentrations without digitalis toxicity.

• 出版日期2010-6
• 单位郑州大学