Research Article

Synthesis and Biological Evaluation of Novel Jatrorrhizine Derivatives with Amino Groups Linked at the 3-Position as Inhibitors of Acetylcholinesterase

Table 1

In vitro inhibition IC50 (µM) and selectivity of jatrorrhizine derivatives for AChE and BuChE.

CompoundsIC50 (µM)Selectivity for

Jatrorrhizine>100>115
Tacrine0.23
3a>100>216
3b>100>260
3c>100>310
3d>100>243
3e >100>338
3f >100>121
3g>100>300

% inhibitory concentration (means ± SEM of three experiments) of AChE from electric eel; % inhibitory concentration (means ± SEM of three experiments) of BuChE from equine serum; for AChE = IC50 (BuChE)/IC50 (AChE).