Novel nonquaternary reactivators showing reactivation efficiency for soman-inhibited human acetylcholinesterase

• Published in: Toxicology letters Vol. 246; pp. 1 - 6
• Main Authors: Wei, Zhao, Liu, Yan-qin, Wang, Yong-an, Li, Wan-hua, Zhou, Xin-bo, Zhao, Jian, Huang, Chun-qian, Li, Xing-zhou, Liu, Jia, Zheng, Zhi-bing, Li, Song
• Format: Journal Article
• Language: English
• Published: Netherlands Elsevier Ireland Ltd 30.03.2016
• Subjects: Acetylcholinesterase; Activation; Blood-Brain Barrier; Cholinesterase Inhibitors - poisoning; Cholinesterase Reactivators - chemical synthesis; Cholinesterase Reactivators - pharmacology; Dual-site binding; Humans; In vitro testing; Ligands; Nonquaternary reactivators; Oximes; Oximes - pharmacokinetics; Oximes - pharmacology; Peripheral site ligand; Poisoning; Pyridinium Compounds - pharmacokinetics; Pyridinium Compounds - pharmacology; Reactivation; Soman; Soman - poisoning; Strategy; Toxicology; AChE; Reactivation; BBB; DTNB; Dual-site binding; ACh; ATCh; A-site; PSL; CNS; TLC; Acetylcholinesterase; BSA; Peripheral site ligand; P-site; Nonquaternary reactivators; Soman

•We designed and synthesized a series of new nonquaternary oximes aiming for reactivation of OP-poisoned hAChE.•Some of these new oximes showed obvious in vitro reactivation potency of soman-inhibited hAChE.•Greater affinity of oximes 7b–9b to hAChE might partially account for their higher reactivat...