Tacrine, Trolox and Tryptoline as Lead Compounds for the Design and Synthesis of Multi-target Agents for Alzheimer’s Disease Therapy

Table 1: In vitro IC₅₀ values of test compounds 8a – 8d, 14 and 16 for TcAChE, eqBuChE and DPPH.


Compounds	AChE IC₅₀ (nM)	BuChE IC₅₀ (nM)	(SI)^a	DPPH IC₅₀ (µM)
8a (n = 2)	1530	128.82	11.87	46.23
8b (n = 3)	1530	12.58	121.62	11.48
8c (n = 4)	2200	11.22	196.07	14.38
8d (n = 6)	49.31	4.74	10.40	12.67
14	17.37	3.16	5.49	129.41
16	>100 µM	1698.24	>58.88	125.89
Tacrine	102	14.12	7.22	nd
Donepezil	220	2870	0.08	nd
Trolox	nd	nd	-	17.57

^aBuChE selectivity index = IC₅₀(TcAChE)/IC₅₀(eqBuChE). n.d. = not determined.