. Author manuscript; available in PMC: 2011 May 1.

Published in final edited form as: Bioorg Med Chem Lett. 2010 Mar 3;20(9):2987–2990. doi: 10.1016/j.bmcl.2010.02.102

Table 1.

Anticholinesterase activities and Clog P values of Class 1 and 2 agents.

Class 1 (Ester-Carbonate Series)				Class 2 (Ester Series)

Compound	IC₅₀ (μM)^a	% AChE Recovery^b	Clog P^c	Compound	IC₅₀ (μM)^a	% AChE Recovery^b	Clog P^c
1	1.93 ± 0.64	101 ± 8	7.37	9	24.6 ± 14.5	107 ± 17	6.47
2	1.19 ± 0.20	88 ± 11	7.53	10	25.7 ± 4.9	92 ± 11	6.64
3	1.74 ± 1.01	99 ± 4	6.50	11	>2000	99 ± 5	0.42
4	0.83 ± 0.15	98 ± 3	6.67	12	19.7 ± 1.7	117 ± 13	5.61
5	2.29 ± 0.94	78 ± 2	7.87	13	13.9 ± 0.3	100 ± 1	5.77
6	0.72 ± 0.13	86 ± 1	8.03	14	>1000	93 ± 13	−0.45
7	0.51 ± 0.02	87 ± 11	8.41	15	9.75 ± 0.89	80 ± 2	6.97
8	1.36 ± 0.13	104 ± 23	8.58	16	3.32 ± 0.36	73 ± 4	7.14
				17	230 ± 32	101 ± 6	0.92
				18	2.69 ± 0.15	99 ± 4	7.52
Tacrine HCl	0.055 ± 0.005	95		19	2.66 ± 0.25	90 ± 10	7.68

Source of AChE is electric eel (Electrophorus electricus). Each condition was run in duplicate.

EeAChE was incubated for 30 min with 55 μM inhibitor at 25°C. Enzyme activity was assayed following gel filtration. Values reported are averages of at least two experiments.

Values calculated using ChemBioDraw Ultra 11.0.