Table 1.
In vitro data for novel NSAID-AChEI Conjugates.*
Compound # | IC50 (μM) | Plasma t1/2 (min−1) | Clog P** |
---|---|---|---|
20 | 77.3 ± 9.43 | <5 | −0.09 |
21 | 40.4 ± 3.91 | nd | 5.87 |
22 | 5–15*** | nd | 1.37 |
23 | 51.8 ±16.9 | <5 | 0.41 |
24 | NA | >12 h | 6.38 |
25 | 10.6 ±2.2 | <5 | 1.87 |
26 | NA | nd | −0.95 |
27 | 35–40*** | >12 h | 5.01 |
28 | nd*** | nd | 0.50 |
Galantamine HBr | 1.12±0.31 | −0.33 | |
Pyridostigmine Mimic (Fig. 2) | NA | −3.49 | |
Neostigmine Mimic (Fig. 2) | 4.75 ±0.41 | −2.76 |
NA – not active; nd – not determined.
Clog P calculated using ChemBioDraw Ultra 12.0.
Precise IC50 values could not be obtained due to limits in compound solubility.