title: Digoxin derivatives substituted by alkylidene at the butenolide part.
abstract: 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 HR-MS. Preliminary bioassay shows that some of them have cardiac functions, especially compound 2g that induced a marked increase in myocardial contractility at 10ngml(-1) and 20ngml(-1) concentrations without digitalis toxicity.
authors.affiliation: School of Pharmaceutical Science, Zhengzhou University, Ke Xue Da Dao 100, Zhengzhou 450001, PR China.
authors.forename: Hai-Wei
authors.initials: HW
authors.lastname: Xu
authors.forename: Gai-Zhi
authors.initials: GZ
authors.lastname: Liu
authors.forename: Song-Lin
authors.initials: SL
authors.lastname: Zhu
authors.forename: Guang-Feng
authors.initials: GF
authors.lastname: Hong
authors.forename: Hong-Min
authors.initials: HM
authors.lastname: Liu
authors.forename: Qiong
authors.initials: Q
authors.lastname: Wu
mesh_terms: D015107:4-Butyrolactone / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D000818:Animals; D001681:Biological Assay / Q000379:methods; D004077:Digoxin / Q000031:analogs & derivatives / Q000138:chemical synthesis / Q000494:pharmacology; D006168:Guinea Pigs; D006321:Heart / Q000187:drug effects; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D015394:Molecular Structure; D013055:Spectrophotometry, Infrared
chemical_list: D004077:Digoxin; C004511:butenolide; D015107:4-Butyrolactone