New oxime reactivators connected with CH₂O(CH₂)_nOCH₂ linker and their reactivation potency for organophosphorus agents-inhibited acetylcholinesterase

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• 作者：Garp Yeol Yang ; Kyung-Ae Oh ; No-Joong Park ; Young-Sik Jung
• 关键词：Organophosphorus agents ; Bis-pyridinium oxime reactivators ; Acetylcholinesterase ; Linker ; Pesticide
• 刊名：Bioorganic and Medicinal Chemistry
• 出版年：2007
• 出版时间：15 December 2007
• 年：2007
• 卷：15
• 期：24
• 页码：7704-7710
• 全文大小：177 K

文摘

New bis-pyridinium oxime reactivators 6 with CH₂O(CH₂)₂OCH₂ and CH₂O(CH₂)₄OCH₂ linkers between the two pyridinium rings were designed and synthesized. In the in vitro test of their potency to reactivate AChE inhibited by organophosphorus agents at 5 × 10⁻³ M concentration, the reactivation ability of 1,2-dimethoxy-ethylene-bis-N,N′-4-pyridiumaldoxime dichloride (6a) was 63 % for housefly (HF) AChE inhibited by diisopropyl fluorophosphates (DFP), 51 % for bovine red blood cell (RBC) AChE inhibited by DFP, 67 % for HF-AChE inhibited by paraoxon, and 81 % for RBC-AChE inhibited by paraoxon. Except in the case of DFP-inhibited HF AChE test of 2-PAM, the activities of 6a are much higher than the activities of 2-PAM and HI-6 which are AChE reactivators currently in use.