Table 3.
Exploring the Role of the Benzylamine Group. Ratio (spontaneous/compound) of half-times (t1/2) of reactivation for compounds (1mM) with RHuAChE after inhibition by the indicated agent.
|
|
|
|
Inhibition of RHuAChE @ 1mM | ||
|---|---|---|---|---|---|---|
| GB | GF | VX | VR | |||
| 1 |
|
361* (158–824) | 164* (97.3–277) | 1,069* (393.6–2911) | 14,723* (6.46–33,573,761) | 60% (±1) |
| 6 |
|
1.97* (1.54–2.52) | 1.80* (1.46–2.22) | 2.76* (1.95–3.93) | 4.06* (3.01–5.49) | 1% (±4) |
| 7 |
|
--- | --- | --- | --- | 95% (±1) |
| 8 |
|
2.13* (1.63–2.78) | 1.96* (1.92–2.01) | 2.72* (2.12–3.48) | 5.65* (1.20–26.5) | 18% (±6) |
| 9 |
|
--- | --- | --- | --- | 94% (±1) |
| 10 |
|
0.88 (0.65–1.20) | 0.74 (0.60–0.90) | 1.09 (0.60–1.98) | 0.93 (0.76–1.14) | 9% (±4) |
---Reactivation could not be determined due to high level of inhibition by compound.