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. 2021 Aug 12;26(16):4895. doi: 10.3390/molecules26164895

Table 2.

AChE and BuChE inhibitory activity of the quinoxaline derivatives.

graphic file with name molecules-26-04895-i001.jpg
Code R R1 R2 IC50
AChE (µM)
IC50
BChE (µM)(%Inhibition)
Selectivity
BChE/AChE
3a H H H 13.22 ± 4.1 40.64 ± 1.6 3.07
3b H Ph H 50.08 ± 2.6 14.91 ± 2.6 0.29
3c H CH3 CH3 7.25 ± 1.5 (23.42 ± 1.7%) -
4a Cl H H 23.87 ± 1.3 (37.42 ± 2.3%) -
4b Cl Ph H 28.49 ± 1.6 (41.16 ± 1.5%) -
4c Cl CH3 CH3 10.67 ± 1.4 (37.35 ± 1.3%) -
5a NO2 H H 21.31 ± 1.5 42.02 ± 1.0 1.97
5b NO2 Ph H 39.0 ± 0.8 60.95 ± 3.4 1.56
5c NO2 CH3 CH3 8.42 ± 1.8 (32.13 ± 1.9%) -
6a NH2 H H 0.74 ± 0.5 (32.87 ± 2.8%) -
6b NH2 Ph H 1.31 ± 0.2 (44.14 ± 1.0%) -
6c NH2 CH3 CH3 0.077 ± 0.01 (29.22 ± 1.95%) -
Tacrine 0.11 ± 0.01 0.0066 ± 0.001 0.09
Galanthamine 0.59 ± 0.13 11.55 ± 5.5 19.58

IC50 values are expressed as the mean ± SD (n = three independent experiments). %inhibition at 100 µM are shown in square brackets as the mean ± SD (n = three independent experiments). Selectivity index for AChE: IC50 BChE/IC50 AChE.