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Table 2 Inhibition of AChE and BuChE activities of title compounds

From: Synthesis and biological evaluation of 1, 3-dihydroxyxanthone mannich base derivatives as anticholinesterase agents

Compd. R3 IC50 (μM) a for AChE IC50 (μM) for BuChE Selectivity for BuChE/AChE
1a H 106.72 ± 5.78 62.93 ± 0.84 0.59
1b H 73.72 ± 1.36 36.98 ± 0.56 0.50
1c H 81.92 ± 2.04 35.49 ± 1.68 0.43
1d H 79.34 ± 5.78 42.98 ± 1.76 0.54
1e H 95.35 ± 1.70 >100 >1.05
2a CH3 2.34 ± 0.20 10.89 ± 0.20 4.66
2b CH3 2.40 ± 0.49 6.79 ± 0.56 2.83
2c CH3 4.20 ± 0.29 7.21 ± 0.75 1.72
2d CH3 7.00 ± 0.07 10.62 ± 0.22 1.53
2e CH3 7.76 ± 2.36 >100 >12.89
3a 5.84 ± 1.19 4.66 ± 0.64 0.80
3b 6.00 ± 0.33 1.54 ± 0.14 0.26
3c 4.36 ± 0.58 3.05 ± 0.13 0.70
3d 3.70 ± 0.16 1.73 ± 0.08 0.47
3e 74.73 ± 4.07 >100 >1.34
4a 2.63 ± 0.07 1.49 ± 0.03 0.57
4b 2.60 ± 0.13 0.51 ± 0.01 0.20
4c 5.85 ± 0.32 2.89 ± 0.07 0.49
4d 55.34 ± 8.15 5.61 ± 0.08 0.10
4e 24.16 ± 0.40 8.83 ± 0.36 0.37
Galanthamine · HBr    1.12 ± 0.02 29.99 ± 0.05 26.78
  1. aData are means ± standard deviation of triplicate independent experiments.