Table 1.
Reactivation results of commercial, formerly published and newly prepared AChE reactivators.
| Non-Reactivating Moiety | GA-HssAChE Reactivation (% ± SD) | POX-HssAChE Reactivation (% ± SD) | MePOX-HssAChE Reactivation (% ± SD) | DFP-HssAChE Reactivation (% ± SD) | HssAChE IC50 ± SD | |||||
|---|---|---|---|---|---|---|---|---|---|---|
| Compound | 100 μM | 10 μM | 100 μM | 10 μM | 100 μM | 10 μM | 100 μM | 10 μM | µM | |
| 1 (2-PAM) | - | 3.3 ± 0.5 | 2.4 ± 0.2 | 10.7 ± 0.3 | 2.1 ± 0.1 | 30.2 ± 0.3 | 22.4 ± 0.7 | 1.3 ± 0.6 | 0.1 ± 0.4 | 878 ± 171 |
| 2 (HI-6) | CONH2 | 0.9 ± 0.6 | 0.8 ± 0.3 | 6.2 ± 0.6 | 1.7 ± 0.1 | 13.6 ± 0.2 | 17.9 ± 0.4 | 0.7 ± 0.1 | 1.4 ± 0.1 | 203 ± 39 |
| 3 (obidoxime) | CH=NOH | 15.1 ± 0.9 | 7.9 ± 0.5 | 59.7 ± 1.0 | 22.4 ± 0.4 | 61.7 ± 0.3 | 45.3 ± 0.9 | 7.6 ± 0.7 | 3.3 ± 0.4 | 577 ± 113 |
| 4 (trimedoxime) | CH=NOH | 31.5 ± 1.2 | 16.9 ± 0.2 | 44.3 ± 0.6 | 22.5 ± 1.3 | 51.4 ± 0.9 | 59.5 ± 0.7 | 10.0 ± 0.5 | 2.7 ± 0.3 | 167 ± 33 |
| 5 (methoxime) | CH=NOH | 2.9 ± 0.01 | 2.1 ± 0.5 | 16.1 ± 0.5 | 1.8 ± 0.3 | 14.2 ± 0.1 | 14.3 ± 0.2 | 2.4 ± 0.1 | 0.6 ± 0.3 | 2010 ± 391 |
| 6 (K048) | CONH2 | 27.4 ± 1.1 | 10.0 ± 0.6 | 25.7 ± 0.7 | 12.5 ± 0.2 | 54.4 ± 0.9 | 29.1 ± 0.4 | 3.8 ± 0.1 | 1.4 ± 0.1 | 349 ± 68 |
| 7 (K074) | CH=NOH | 32.1 ± 0.6 | 24.6 ± 0.2 | 31.1 ± 0.4 | 13.9 ± 0.8 | 17.9 ± 0.1 | 21.2 ± 0.4 | 1.4 ± 0.5 | 1.4 ± 0.2 | 29 ± 6 |
| 8 (K075) | CH=NOH | 19.5 ± 1.0 | 18.1 ± 0.2 | 28.5 ± 1.1 | 14.1 ± 0.3 | 19.2 ± 0.9 | 22.8 ± 0.2 | 1.1 ± 0.3 | 1.5 ±0.2 | 80 ± 16 |
| 9 (K203) | CONH2 | 48.1 ± 1.5 | 21.2 ± 0.3 | 39.3 ± 0.4 | 13.1 ± 0.4 | 55.9 ± 0.5 | 41.1 ± 0.1 | 4.4 ± 0.1 | 2.1 ± 0.4 | 566 ± 110 |
| 10 | pyridinium | 3.9 ± 0.1 | 4.5 ± 0.3 | 16.6 ± 1.0 | 3.5 ± 0.3 | 14.3 ± 0.8 | 13.2 ± 0.1 | 2.4 ± 0.5 | 0.4 ± 0.3 | - |
| 11 | pyridazinium | 1.5 ± 0.5 | 4.1 ± 0.2 | 6.3 ± 0.8 | 3.0 ± 0.3 | 7.1 ± 0.7 | 11.8 ± 0.4 | 1.2 ± 0.7 | 1.0 ± 0.4 | - |
| 12 | quinolinium | 0.6 ± 0.4 | 3.1 ± 0.3 | 0.6 ± 0.5 | 2.0 ± 0.1 | 2.2 ± 0.5 | 8.6 ± 0.4 | 0.2 ± 1.0 | 0.8 ± 0.2 | - |
| 13 | isoquinolinium | 3.5 ± 0.7 | 6.0 ± 0.2 | 9.1 ± 0.3 | 8.7 ± 0.3 | 8.2 ± 0.8 | 16.9 ± 0.4 | 0.7 ± 0.2 | 1.1 ± 0.2 | - |
| 14 | Me | 3.4 ± 0.4 | 6.3 ± 0.3 | 24.5 ± 0.3 | 7.6 ± 0.6 | 9.5 ± 0.5 | 9.4 ± 0.2 | 1.1 ± 0.4 | 0.8 ± 0.3 | - |
| 15 | tBut | 1.7 ± 0.4 | 3.9 ± 0.3 | 18.7 ± 0.2 | 58.7 ± 4.0 | 4.0 ± 0.5 | 7.6 ± 0.5 | 1.7 ± 0.5 | 0.8 ± 0.3 | 24 ± 6 |
| 16 | Ph | 0.7 ± 0.4 | 3.5 ± 0.3 | 6.9 ± 0.4 | 8.9 ± 0.5 | 1.7 ± 0.3 | 6.2 ± 0.4 | 0.7 ± 0.2 | 1.0 ± 0.3 | 6 ± 1 |
| 17 | Bn | 0.3 ± 0.2 | 1.9 ± 0.6 | 1.2 ± 0.1 | 4.7 ± 0.3 | 0.0 ± 0.1 | 3.8 ± 0.4 | 0.0 ± 0.5 | 0.8 ± 0.2 | - |
| 18 | CH2OH | 2.6 ± 0.3 | 4.0 ± 0.3 | 20.6 ± 0.1 | 8.0 ± 0.1 | 6.7 ± 0.3 | 8.1 ± 0.3 | 3.8 ± 1.0 | 1.4 ± 0.4 | - |
| 19 | COMe | 1.7 ± 0.3 | 3.1 ± 0.1 | 11.9 ± 1.0 | 3.9 ± 0.3 | 5.2 ± 0.4 | 7.5 ± 0.1 | 1.5 ± 0.3 | 1.0 ± 0.2 | - |
| 20 | COOH | 3.3 ± 0.5 | 6.2 ± 0.3 | 14.5 ± 0.6 | 4.2 ± 0.4 | 9.5 ± 0.3 | 8.8 ± 0.4 | 1.1 ± 0.5 | 0.4 ± 0.1 | - |
| 21 | COOEt | 1.7 ± 0.5 | 4.1 ± 0.2 | 7.1 ± 0.7 | 4.0 ± 0.6 | 3.8 ± 0.4 | 7.2 ± 0.2 | 0.8 ± 0.3 | 1.1 ± 0.2 | - |
| 22 | CN | 3.6 ± 0.4 | 5.2 ± 0.2 | 10.1 ± 0.8 | 42.6 ± 0.1 | 11.1 ± 0.1 | 13.8 ± 0.3 | 1.7 ± 0.5 | 0.4 ± 0.2 | 45 ± 9 |
| 23 | C(NH2)=NOH | 12.8 ± 0.9 | 13.1 ± 0.4 | 19.1 ± 0.8 | 7.4 ± 0.3 | 20.2 ± 1.0 | 20.7 ± 0.4 | 3.1 ± 0.8 | 2.0 ± 0.2 | 90 ± 17 |
| 24 | 3,4-CONH2 | 1.8 ± 0.6 | 4.5 ± 0.2 | 2.0 ± 0.4 | 2.2 ± 0.8 | 4.2 ± 0.5 | 10.1 ± 0.2 | 0.7 ± 0.4 | 0.7 ± 1.0 | - |