Table 1 Structure and potency of previously reported anti-AD candidates

A

hAChE IC₅₀ = 0.361 µM vs donepezil with IC₅₀ = 0.006 ± 0.001 µM

hBChE IC₅₀ > 1000 µM vs donepezil with IC₅₀ = 1.830 ± 0.176 µM

PAMPA-BBB =  + vs progesterone with PAMPA-BBB =  + 

B

AChE IC₅₀ = 3.33 µM vs donepezil with IC₅₀ = 0.011 ± 0.0002 µM

BChE = 14.1% ± 5.8 at 10 µM vs donepezil with IC₅₀ = 1.83 ± 0.04 µM

hBACE-1 = 43.7% inhibition at 50 µM vs calbiochem with IC₅₀ = 0.046, Aß-aggregation = 24.9% inhibition at 10 µM vs resveratrol with 78.5% ± 5.2 inhibition

c

AChE IC₅₀ = 53.1 ± 4.56 µM vs donepezil with IC₅₀ = 23 nM

BChE IC₅₀ = 67.3 ± 5.24 µM vs donepezil with IC₅₀ = 7.4 µM

D

AChE IC₅₀ = 0.0465 µM vs neostigmine with IC₅₀ = 0.136 µM

BChE IC₅₀ = 0.0702 µM vs neostigmine with IC₅₀ = 0.084 µM