Table 1.

Acetylcholinesterase inhibitory activity of 3-aminocoumarin derivatives.

structure	compound	R	X	n	IC50 (nM) ± SDa,b
	3	H	–	–	12%c
	8	OMe	–	–	5%c
	4	H	–	0	0%c
	5	H	–	1	8%c
	9	OMe	–	0	9%c
	10	OMe	–	1	9%c
	4a	H	H	0	71.88 ± 3.44
	5a	H	H	1	10%c
	9a	OMe	H	0	12.48 ± 0.71
	10a	OMe	H	1	1087.7 ± 0.05
	9b	OMe	2-Cl	0	6.03 ± 0.18
	9c	OMe	3-Cl	0	11.47 ± 0.63
	9d	OMe	4-Cl	0	293.17 ± 13.57
	9e	OMe	2-F	0	3.05 ± 0.28
	9f	OMe	3-F	0	5.04 ± 0.26
	9g	OMe	4-F	0	5.31 ± 0.38
	9h	OMe	2,3-di-F	0	1.53 ± 0.01
	9i	OMe	2,6-di-F	0	2.43 ± 0.18
	donepezil·HCl	–	–	–	53.51 ± 3.12
	tacrine	–	–	–	190.37 ± 4.55

^aConcentration of the compound that produced 50% inhibition of enzyme activity.

^bResults are expressed as mean ± standard error with the average of triplicate independent experiments.

^c% Inhibition at concentration of 1 μM.