Table 1.

Inhibition (IC₅₀ values in µM, with standard error) of the activity of EeAChE (from Electrophorus electricus) and BChE (from Equus ferus) by donepezil and its analogues 7 and 8a–v, and the selectivity index (SI) for each inhibitor based on IC₅₀ values.

Cpd	EeAChE	EfBChE	SI
Donepezil HCl	0.12 ± 0.01	2.0 ± 0.1	17
7	0.41 ± 0.05	4.3 ± 0.4	11
8a	0.054 ± 0.003	0.57 ± 0.04	11
8b	0.021 ± 0.003	0.48 ± 0.03	23
8c	0.14 ± 0.02	2.1 ± 0.3	15
8d	0.059 ± 0.004	1.3 ± 0.1	22
8e	0.044 ± 0.003	1.3 ± 0.2	30
8f	0.061 ± 0.007	1.3 ± 0.2	21
8g	0.79 ± 0.28	5.2 ± 1.6	6.6
8h	0.13 ± 0.01	0.70 ± 0.05	5.4
8i	0.23 ± 0.03	1.0 ± 0.2	4.3
8j	0.13 ± 0.01	0.67 ± 0.17	5.2
8k	0.13 ± 0.02	0.46 ± 0.06	3.5
8l	0.071 ± 0.015	0.72 ± 0.10	10
8m	0.081 ± 0.005	0.57 ± 0.10	7.0
8n	0.16 ± 0.02	0.96 ± 0.15	6.0
8o	0.12 ± 0.02	0.76 ± 0.12	6.3
8p	0.032 ± 0.010	0.25 ± 0.08	7.8
8q	0.11 ± 0.01	0.48 ± 0.08	4.4
8r	0.090 ± 0.009	0.60 ± 0.15	6.7
8s	0.016 ± 0.001	0.44 ± 0.05	28
8t	0.054 ± 0.007	0.37 ± 0.05	6.9
8u	0.027 ± 0.004	0.20 ± 0.03	7.4
8v	0.17 ± 0.02	0.11 ± 0.01	0.69