Potent acetylcholinesterase inhibitors: design, synthesis and structure–activity relationships of alkylene linked bis-galanthamine and galanthamine–galanthaminium salts

Screening of Non‐Alkaloidal Natural Compounds as Acetylcholinesterase Inhibitors

“…Since Methods I and IV gave similar values, the former as the easier and faster of the two was used for all K i calculations. The K c i value so obtained is in agreement with an IC 50 value of 0.36 mm reported for the inhibition of Electrophorus electricus AChE by galanthamine [21]. The method was also validated with a variety of additional compounds [22] acting according to other inhibition types (results not shown).…”

Discovery of drug candidates from some Turkish plants and conservation of biodiversity

“…Although the most common side effect of galanthamine is nausea, it is possible to eliminate nausea by increasing the galanthamine dose slowly [33]. In addition, galanthamine was shown to have no hepatotoxicity [34]. Therefore, galanthamine (Nivalin ® ) has been approved as its HBr salt for the first time in Austria, later licensed as Reminyl ® in the United States and some European countries, as well as Turkey.…”

Structure-activity relationship study of diterpenes for treatment of Alzheimer’s disease

“…26 Other galantamine derivatives bearing this allylic hydroxyl group were also reported as potent AChE inhibitors. 27 The presence of the acetoxy group at C-15 in 4 may be responsible for decreasing the activity (65.0 ± 4.5%) of this natural product when compared to 1 (81.6 ± 1.8). It is worth mentioning that the biological activity of compound 6 (54.6 ± 4.0%), derived from 4 by esterification at C-19, was even lower.…”