Table 11. hMAO Inhibitory Activity of Donepezil–Trolox Hybrids.

compound	n	R	IC50 for MAO-A (μM)	IC50 for MAO-B (μM)	SI valuea
113	0	4-OCH3	15.3 ± 0.2	2.5 ± 0.1	6.12
114	0	2-CH3	13.1 ± 0.3	3.1 ± 0.2	4.225
115	0	4-CH3	12.7 ± 0.3	3.3 ± 0.2	3.848
116	0	2-F	8.9 ± 0.1	1.7 ± 0.2	5.235
117	0	3-F	9.3 ± 0.2	1.6 ± 0.3	5.812
118	0	4-F	11.4 ± 0.1	1.8 ± 0.3	6.333
119	0	2,4-2F	11.8 ± 1.2	1.9 ± 0.2	6.210
120	0	3,4-2F	12.5 ± 1.5	2.3 ± 0.5	5.434
121	0	2-Cl	12.7 ± 2.1	1.7 ± 0.3	7.470
122	0	3-Cl	13.8 ± 1.5	3.1 ± 0.1	4.451
123	0	4-Br	12.6 ± 0.3	2.7 ± 0.9	4.666
124	0	4-NO2	13.2 ± 0.5	1.9 ± 0.3	6.947
125	0	H	11.1 ± 0.4	3.2 ± 0.3	3.468
126	2	4-OCH3	7.8 ± 0.6	7.3 ± 0.2	1.068
127	2	2-CH3	8.4 ± 0.1	6.9 ± 0.1	1.217
128	2	4-CH3	8.9 ± 0.1	7.5 ± 0.1	1.186
129	2	2-F	4.4 ± 0.2	4.3 ± 0.2	1.023
130	2	3-F	5.3 ± 0.5	4.6 ± 0.2	1.152
131	2	4-F	4.8 ± 0.1	4.5 ± 0.3	1.066
132	2	2,4-2F	5.7 ± 0.3	5.8 ± 1.0	0.982
133	2	3,4-2F	8.1 ± 0.2	5.3 ± 0.7	1.528
134	2	2-Cl	7.2 ± 0.4	6.1 ± 0.4	1.180
135	2	3-Cl	5.8 ± 0.5	4.8 ± 0.3	1.208
136	2	4-Br	6.3 ± 0.2	5.7 ± 0.2	1.105
137	2	4-NO2	5.4 ± 0.2	4.9 ± 0.1	1.102
138	2	H	5.6 ± 0.2	5.1 ± 0.2	1.098

^aSelectivity index for MAO-B (IC₅₀ for MAO-A/IC₅₀ for MAO-B).