ArticleJournal of medicinal chemistry2014
Imidazole aldoximes effective in assisting butyrylcholinesterase catalysis of organophosphate detoxification.
Article in Journal of medicinal chemistry, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 26 papers.
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Who cites it
26 citing papers in PubMed, 82 citations in OpenAlex.
- Next-generation broad-spectrum reactivators for effective countermeasure against organophosphorus poisoning.Archives of toxicology · 2026Article
- Click-chemistry-derived oxime library reveals efficient reactivators of nerve agent-inhibited butyrylcholinesterase suitable for pseudo-catalytic bioscavenging.Archives of toxicology · 2025Article
- New Heterostilbene and Triazole Oximes as Potential CNS-Active and Cholinesterase-Targeted Therapeutics.Biomolecules · 2024Article
- Advancements in bioscavenger mediated detoxification of organophosphorus poisoning.Toxicology research · 2024Review
- Structural and dynamic effects of paraoxon binding to human acetylcholinesterase by X-ray crystallography and inelastic neutron scattering.Structure (London, England : 1993) · 2022Article
- Discovery of Novel Non-Oxime Reactivators Showing In Vivo Antidotal Efficiency for Sarin Poisoned Mice.Molecules (Basel, Switzerland) · 2022Article
- Clinical Analysis of Acute Organophosphorus Pesticide Poisoning and Successful Cardiopulmonary Resuscitation: A Case Series.Frontiers in public health · 2022Article
- Design, synthesis,Journal of enzyme inhibition and medicinal chemistry · 2021Article
- Development of a CNS-permeable reactivator for nerve agent exposure: an iterative, multi-disciplinary approach.Scientific reports · 2021Article
- Non-quaternary oximes detoxify nerve agents and reactivate nerve agent-inhibited human butyrylcholinesterase.Communications biology · 2021Article
- Development of versatile and potent monoquaternary reactivators of acetylcholinesterase.Archives of toxicology · 2021Article
- Nanomaterial-Enabled Sensors and Therapeutic Platforms for Reactive Organophosphates.Nanomaterials (Basel, Switzerland) · 2021Review
- Counteracting poisoning with chemical warfare nerve agents.Arhiv za higijenu rada i toksikologiju · 2020Review
- Organophosphorus compounds and oximes: a critical review.Archives of toxicology · 2020Review
- Positron emission tomography studies of organophosphate chemical threats and oxime countermeasures.Neurobiology of disease · 2020Review
- Tuning Butyrylcholinesterase Inactivation and Reactivation by Polymer-Based Protein Engineering.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2020Article
- In Vitro Evaluation of Neutral Aryloximes as Reactivators forBiomolecules · 2019Article
- Productive reorientation of a bound oxime reactivator revealed in room temperature X-ray structures of native and VX-inhibited human acetylcholinesterase.The Journal of biological chemistry · 2019Article
- A Candidate for Multitopic Probes for Ligand Discovery in Dynamic Combinatorial Chemistry.Molecules (Basel, Switzerland) · 2019Article
- Resurrection and Reactivation of Acetylcholinesterase and Butyrylcholinesterase.Chemistry (Weinheim an der Bergstrasse, Germany) · 2019Review
Corrections and comments
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Authors and funding
6 authors at 3 institutions in 2 countries.
Funding
Abstract
Intoxication by organophosphate (OP) nerve agents and pesticides should be addressed by efficient, quickly deployable countermeasures such as antidotes reactivating acetylcholinesterase or scavenging the parent OP. We present here synthesis and initial in vitro characterization of 14 imidazole aldoximes and their structural refinement into three efficient reactivators of human butyrylcholinesterase (hBChE) inhibited covalently by nerve agent OPs, sarin, cyclosarin, VX, and the OP pesticide metabolite, paraoxon. Rapid reactivation of OP-hBChE conjugates by uncharged and nonprotonated tertiary imidazole aldoximes allows the design of a new OP countermeasure by conversion of hBChE from a stoichiometric to catalytic OP bioscavenger with the prospect of oral bioavailability and central nervous system penetration. The enhanced in vitro reactivation efficacy determined for tertiary imidazole aldoximes compared to that of their quaternary N-methyl imidazolium analogues is attributed to ion pairing of the cationic imidazolium with Asp 70, altering a reactive alignment of the aldoxime with the phosphorus in the OP-hBChE conjugate.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.