The present armamentarium of commercially available antidotes provides limited protection against the neurological effects of organophosphate exposure. Hence, there is an urgent need to design and develop molecules that can protect and reactivate inhibited-AChE in the central nervous system. Some natural compounds like glucose and certain amino acids (glutamate, the anion of glutamic acid) can easily cross the blood brain barrier although they are highly polar. Glucose is mainly transported by systems like glucose transporter protein type 1 (GLUT1). For this reason, a series of non-quaternary and quaternary glycosylated imidazolium oximes with different alkane linkers have been designed and synthesized. These compounds were evaluated for their in-vitro reactivation ability against pesticide (paraoxon-ethyl and paraoxon-methyl) inhibited-AChE and compared with standards antidote AChE reactivators pralidoxime and obidoxime. Several physicochemical properties including acid dissociation constant (pK_a), logP, logD, HBD and HBA, have also been assessed for reported compounds. Out of the synthesized compounds, three have exhibited comparable potency with a standard antidote (pralidoxime).

市售解毒剂的当前装备库对有机磷暴露的神经学作用提供了有限的保护。因此，迫切需要设计和开发可以保护和重新激活中枢神经系统中受抑制的AChE的分子。某些天然化合物，例如葡萄糖和某些氨基酸（谷氨酸盐，谷氨酸的阴离子），尽管极性很高，但很容易穿过血脑屏障。葡萄糖主要通过1型葡萄糖转运蛋白（GLUT1）等系统转运。因此，已经设计并合成了具有不同烷烃连接基的一系列非季铵和季铵糖基化的咪唑肟。对这些化合物进行了体外评估对农药（对氧磷乙基和对氧磷甲基）具有抑制AChE的重活化能力，并与标准解毒剂AChE活化剂普利昔肟和obidoxime相比。还针对报告的化合物评估了一些物理化学性质，包括酸解离常数（p K _a），log P，log D，HBD和HBA。在合成的化合物中，三种显示出与标准解毒剂（普利昔肟）相当的效力。