A new series of nonquaternary conjugates for reactivation of both nerve agents and pesticides inhibited hAChE were described in this paper. It was found that substituted salicylaldehydes conjugated to aminobenzamide through piperidine would produce efficient reactivators for sarin, VX and tabun inhibited hAChE, such as L6M1R3, L6M1R5 to L6M1R7, L4M1R3 and L4M1R5 to L4M1R7. The in vitro reactivation experiment for pesticides inhibited hAChE of these new synthesized oximes were conducted for the first time. Despite they were less efficient than obidoxime, some of them were highlighted as equal or more efficient reactivators in comparison to 2-PAM. It was found that introduction of peripheral site ligands could increase oximes’ binding affinity for inhibited hAChE in most cases, which resulted in greater reactivation ability.

本文描述了一系列新的非季铵盐共轭物，用于神经活性剂和农药抑制hAChE的活化。发现通过哌啶与氨基苯甲酰胺缀合的取代的水杨醛将产生沙林，VX和塔宾抑制的hAChE的有效活化剂，例如L6M1R3，L6M1R5至L6M1R7，L4M1R3和L4M1R5至L4M1R7。在体外首次进行了农药抑制hAChE的复活实验。尽管它们的效率不如奥比多肟，但与2-PAM相比，它们中的一些被认为是同等或更有效的再活化剂。发现在大多数情况下，引入外围位点配体可以增加肟对抑制的hAChE的结合亲和力，从而导致更大的再活化能力。