https://orcid.org/0000-0003-3382-3997
Figures & data
Figure 1. Structure of commercially available oxime reactivators.
Figure 2. Structure of K027 (5), K048 (6) and K203 (7).
Scheme 1. Synthesis of bisquaternary salts K487 (11), K488 (12) and K489 (13). Reagents and conditions: (a) 4-pyridinethioamide, DMF, 60 °C, 48 h, yields: 36% (for 11), 52% (for 12), 61% (for 13).
Figure 3. Stability of tested compounds in unionised water (A) and in PBS (B) at 37 °C.
Table 1. The pKa values of tested compounds and parent oximes.
Figure 4. Inhibitory effect of tested compounds on hrAChE (A) and hrBChE (B).
Figure 5. Reactivation of hrAChE inhibited by OP surrogates (%) with 10 µM oximes 11–13 after 15 min at 37 °C. Results were compared to pralidoxime (1), asoxime (4) and parent oximes (5–7).
Figure 6. Reactivation of hrBChE inhibited by OP surrogates (%) with 100 µM oximes 11–13 after 15 min at 37 °C. Results were compared to pralidoxime (1), asoxime (4) and parent oximes (5–7).
Figure 7. Reactivation kinetics of K027 (5) and K487 (11) of hrAChE-NEDPA (A) and hrBChE-NIMP (B).
Table 2. Reactivation kinetic parameters of tested compounds.