FIGURE 1.
Reactivation of VX-, cyclosarin-, sarin-, and paraoxon-inhibited hAChE by library of 134 uncharged oxime reactivators. Reactivation rates (kobs) of 0.67 mm oximes (measured at 37 °C in 0.10 m phosphate buffer, pH 7.4) are given relative to 2PAM. Average reactivation potencies of oximes for all four organophosphates are shown as green bars. Oxime IDs are ordered by their average reactivity (A), segregated by their general structure as acetamide, imidazole, and other oximes (B), and segregated by length of a linker connecting an oxime nucleophile and part of the molecule “R” responsible for binding interaction with hAChE (C). Measured rates of oximolysis (3 × DA/min) and calculated fractions of oximate anion for pH 7.4 are also given as black and gray bars, respectively. Structures and reactivation potencies of all 134 oximes are given in supplemental Table S1.