Design, evaluation and structure—Activity relationship studies of the AChE reactivators against organophosphorus pesticides

K Musilek, M Dolezal, F Gunn‐Moore… - Medicinal research …, 2011 - Wiley Online Library
Organophosphate pesticides (OPPs; eg chlorpyrifos, diazinon, paraoxon) are a wide and
heterogeneous group of organophosphorus compounds. Their biological activity of …

Trends in the recent patent literature on cholinesterase reactivators (2016–2019)

AA de Castro, LC Assis, FV Soares, K Kuca, DA Polisel… - Biomolecules, 2020 - mdpi.com
Acetylcholinesterase (AChE) is the key enzyme responsible for deactivating the ACh
neurotransmitter. Irreversible or prolonged inhibition of AChE, therefore, elevates synaptic …

Pyridinium Oximes with Ortho-Positioned Chlorine Moiety Exhibit Improved Physicochemical Properties and Efficient Reactivation of Human Acetylcholinesterase …

T Zorbaz, D Malinak, N Maraković… - Journal of medicinal …, 2018 - ACS Publications
Six chlorinated bispyridinium mono-oximes, analogous to potent charged reactivators K027,
K048, and K203, were synthesized with the aim of improving lipophilicity and reducing the p …

Activation of (un) regulated cell death as a new perspective for bispyridinium and imidazolium oximes

A Zandona, N Maraković, P Mišetić, J Madunić… - Archives of …, 2021 - Springer
Oximes, investigated as antidotes against organophosphates (OP) poisoning, are known to
display toxic effects on a cellular level, which could be explained beyond action on …

Investigation of the reactivation kinetics of a large series of bispyridinium oximes with organophosphate-inhibited human acetylcholinesterase

M Winter, T Wille, K Musilek, K Kuca, H Thiermann… - Toxicology Letters, 2016 - Elsevier
The limited effectiveness of the established oximes obidoxime and pralidoxime resulted in
ongoing research on novel oximes for the reactivation of acetylcholinesterase (AChE) …

An evaluation of therapeutic and reactivating effects of newly developed oximes (K156, K203) and commonly used oximes (obidoxime, trimedoxime, HI-6) in tabun …

J Kassa, J Karasova, K Musilek, K Kuca - Toxicology, 2008 - Elsevier
The potency of newly developed monoxime bispyridinium compounds (K156, K203) in
reactivating tabun-inhibited acetylcholinesterase and reducing tabun-induced lethal toxic …

Molecular modeling and in vitro reactivation study between the oxime BI-6 and acetylcholinesterase inhibited by different nerve agents

JOS Giacoppo, T CC França, K Kuča… - Journal of …, 2015 - Taylor & Francis
Nerve agents are organophosphates acting as potent inhibitors of acetylcholinesterase
(AChE), the enzyme responsible for the hydrolysis of acetylcholine and, consequently, the …

Chlorpyrifos removal in an artificially contaminated soil using novel bacterial strains and cyclodextrin. Evaluation of its effectiveness by ecotoxicity studies

A Lara-Moreno, E Morillo, F Merchán, F Madrid… - Agronomy, 2022 - mdpi.com
The removal of chlorpyrifos (CLP) from the environment is a matter of general interest,
because it is one of the most widely used insecticides in the world but presents a high …

Mono-oxime bisquaternary acetylcholinesterase reactivators with prop-1, 3-diyl linkage—Preparation, in vitro screening and molecular docking

K Musilek, M Komloova, O Holas, A Horova… - Bioorganic & medicinal …, 2011 - Elsevier
The treatment of organophosphorus (OP) poisoning consists of the administration of a
parasympatholytic agent (eg, atropine), an anticonvulsant (eg, diazepam) and an …

Reactivation kinetics of 31 structurally different bispyridinium oximes with organophosphate-inhibited human butyrylcholinesterase

G Horn, T Wille, K Musilek, K Kuca, H Thiermann… - Archives of …, 2015 - Springer
Organophosphorus compounds (OP) are bound to human butyrylcholinesterase (BChE) and
endogenous or exogenous BChE may act as a stoichiometric scavenger. Adequate amounts …