Results 11 to 20 of about 411 (95)

Trends in the Recent Patent Literature on Cholinesterase Reactivators (2016–2019) [PDF]

open access: yesBiomolecules, 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
Kamil Kuča   +2 more
exaly   +4 more sources

Pyridinium-2-carbaldoximes with quinolinium carboxamide moiety are simultaneous reactivators of acetylcholinesterase and butyrylcholinesterase inhibited by nerve agent surrogates [PDF]

open access: yesJournal 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   +2 more sources

Molecular Modeling Studies on the Multistep Reactivation Process of Organophosphate-Inhibited Acetylcholinesterase and Butyrylcholinesterase [PDF]

open access: yesBiomolecules, 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   +2 more sources

Design, synthesis, in silico studies and in vitro evaluation of isatin-pyridine oximes hybrids as novel acetylcholinesterase reactivators

open access: yesJournal 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 ...
Kamil Kuča   +2 more
exaly   +2 more sources

New Heterostilbene and Triazole Oximes as Potential CNS-Active and Cholinesterase-Targeted Therapeutics [PDF]

open access: yesBiomolecules
New 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

Effect of Several New and Currently Available Oxime Cholinesterase Reactivators on Tabun-intoxicated Rats [PDF]

open access: yesInternational Journal of Molecular Sciences, 2008
Miroslav Pohanka   +2 more
exaly   +2 more sources

From Mechanisms to Materials: Oximate Reactivity and Emerging Strategies for Organophosphate Detoxification. [PDF]

open access: yesChemphyschem
The development of effective strategies for the detoxification of organophosphorus (OP) nerve agents has evolved from the early mechanistic studies of François Terrier and collaborators, who first elucidated the exceptional nucleophilicity of α‐effect species such as oximes and hydroxamates, to the modern design of supramolecular and material‐based ...
Rodríguez-Dafonte P.
europepmc   +2 more sources

Tuning Butyrylcholinesterase Inactivation and Reactivation by Polymer‐Based Protein Engineering

open access: yesAdvanced 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

Efficacy Assessment of an Uncharged Reactivator of NOP-Inhibited Acetylcholinesterase Based on Tetrahydroacridine Pyridine-Aldoxime Hybrid in Mouse Compared to Pralidoxime

open access: yesBiomolecules, 2020
(1) Background: Human exposure to organophosphorus compounds employed as pesticides or as chemical warfare agents induces deleterious effects due to cholinesterase inhibition. One therapeutic approach is the reactivation of inhibited acetylcholinesterase
André-Guilhem Calas   +18 more
doaj   +1 more source

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