Pyridinium-2-carbaldoximes with quinolinium carboxamide moiety are simultaneous reactivators of acetylcholinesterase and butyrylcholinesterase inhibited by nerve agent surrogates [PDF]
Journal of Enzyme Inhibition and Medicinal Chemistry, 2021 The pyridinium-2-carbaldoximes with quinolinium carboxamide moiety were designed and synthesised as cholinesterase reactivators. The prepared compounds showed intermediate-to-high inhibition of both cholinesterases when compared to standard oximes. Their
Hyun Myung Lee +13 more
doaj +4 more sources
Molecular Modeling Studies on the Multistep Reactivation Process of Organophosphate-Inhibited Acetylcholinesterase and Butyrylcholinesterase [PDF]
Biomolecules, 2021 Poisoning with organophosphorus compounds used as pesticides or misused as chemical weapons remains a serious threat to human health and life.
Jakub Jończyk +6 more
doaj +5 more sources
Trends in the Recent Patent Literature on Cholinesterase Reactivators (2016–2019) [PDF]
Biomolecules, 2020 Acetylcholinesterase (AChE) is the key enzyme responsible for deactivating the ACh neurotransmitter. Irreversible or prolonged inhibition of AChE, therefore, elevates synaptic ACh leading to serious central and peripheral adverse effects which fall under
Alexandre A. de Castro +6 more
doaj +2 more sources
Effect of seven newly synthesized and currently available oxime cholinesterase reactivators on cyclosarin-intoxicated rats. [PDF]
Int J Mol Sci, 2009 Seven new oxime-based acetylcholinesterase reactivators were compared with three currently available ones (obidoxime, trimedoxime, HI-6) for their ability to lessen cholinesterase inhibition in blood and brain of cyclosarin-treated rats.
Karasova JZ +5 more
europepmc +6 more sources
Effect of several new and currently available oxime cholinesterase reactivators on tabun-intoxicated rats. [PDF]
Int J Mol Sci, 2008 The therapeutical efficacies of eleven oxime-based acetylcholinesterase reactivators were compared in an in vivo (rat model) study of treatment of intoxication caused by tabun.
Karasova JZ +5 more
europepmc +4 more sources
Design, synthesis, in silico studies and in vitro evaluation of isatin-pyridine oximes hybrids as novel acetylcholinesterase reactivators [PDF]
Journal of Enzyme Inhibition and Medicinal Chemistry, 2021 Organophosphorus poisoning caused by some pesticides and nerve agents is a life-threating condition that must be swiftly addressed to avoid casualties. Despite the availability of medical countermeasures, the clinically available compounds lack a broad ...
Daniel A. S. Kitagawa +14 more
doaj +2 more sources
The Experimental Oxime K027—A Promising Protector From Organophosphate Pesticide Poisoning. A Review Comparing K027, K048, Pralidoxime, and Obidoxime [PDF]
Frontiers in Neuroscience, 2019 Poisoning with organophosphorus compounds (OPCs) is a major problem worldwide. Standard therapy with atropine and established oxime-type enzyme reactivators (pralidoxime, obidoxime) is unsatisfactory.
Dietrich E. Lorke +2 more
doaj +3 more sources
New Heterostilbene and Triazole Oximes as Potential CNS-Active and Cholinesterase-Targeted Therapeutics [PDF]
BiomoleculesNew furan, thiophene, and triazole oximes were synthesized through several-step reaction paths to investigate their potential for the development of central nervous systems (CNS)-active and cholinesterase-targeted therapeutics in organophosphorus ...
Milena Mlakić +4 more
doaj +2 more sources
Clinical characteristics and treatment of mixed-pesticide poisoning in a patient: reflections on a particular case [PDF]
Journal of International Medical Research, 2020 Patients who commit suicide often deliberately hide their medical history. Given that taking pesticides is one of the most common methods of suicide, other forms of poisoning may be neglected in clinical practice. We report here a case of mixed-pesticide
Yiming Tao +4 more
doaj +2 more sources
Tuning Butyrylcholinesterase Inactivation and Reactivation by Polymer‐Based Protein Engineering
Advanced Science, 2020 Organophosphate nerve agents rapidly inhibit cholinesterases thereby destroying the ability to sustain life. Strong nucleophiles, such as oximes, have been used as therapeutic reactivators of cholinesterase‐organophosphate complexes, but suffer from ...
Libin Zhang +7 more
doaj +1 more source