The value of novel oximes for treatment of poisoning by organophosphorus compounds

F Worek, H Thiermann - Pharmacology & therapeutics, 2013 - Elsevier
Poisoning by organophosphorus compounds (OP) still is a major therapeutic problem.
Intentional OP pesticide poisoning results in up to 300.000 deaths each year and highly …

Cholinesterase reactivators and bioscavengers for pre‐and post‐exposure treatments of organophosphorus poisoning

P Masson, F Nachon - Journal of neurochemistry, 2017 - Wiley Online Library
Organophosphorus agents (OP s) irreversibly inhibit acetylcholinesterase (AC hE) causing a
major cholinergic syndrome. The medical counter‐measures of OP poisoning have not …

Assessment of four organophosphorus pesticides as inhibitors of human acetylcholinesterase and butyrylcholinesterase

T Čadež, D Kolić, G Šinko, Z Kovarik - Scientific reports, 2021 - nature.com
Toxicity of organophosphorus compounds (OPs) remains a major public health concern due
to their widespread use as pesticides and the existence of nerve agents. Their common …

Recent advances in cholinergic mechanisms as reactions to toxicity, stress, and neuroimmune insults

Z Kovarik, G Moshitzky, N Maček Hrvat… - Journal of …, 2024 - Wiley Online Library
This review presents recent studies of the chemical and molecular regulators of
acetylcholine (ACh) signaling and the complexity of the small molecule and RNA regulators …

Counteracting poisoning with chemical warfare nerve agents

N Maček Hrvat, Z Kovarik - Arhiv za higijenu rada i toksikologiju, 2020 - hrcak.srce.hr
Sažetak Phosphylation of the pivotal enzyme acetylcholinesterase (AChE) by nerve agents
(NAs) leads to irreversible inhibition of the enzyme and accumulation of neurotransmitter …

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 …

A newly developed oxime K203 is the most effective reactivator of tabun-inhibited acetylcholinesterase

K Kuca, K Musilek, D Jun, J Zdarova-Karasova… - BMC Pharmacology and …, 2018 - Springer
Background Based on in vitro and in vivo rat experiments, the newly developed
acetylcholinesterase (AChE) reactivator, K203, appears to be much more effective in the …

Modeling of a near-attack conformation of oxime in phosphorylated acetylcholinesterase via a reactivation product, a phosphorylated oxime

G Šinko - Chemico-biological interactions, 2023 - Elsevier
At the present, only four antidotes are in use in therapy for poisoning by organophosphorus
compounds: 2-PAM, HI-6, obidoxime and trimedoxime. Numerous compounds have been …

Centrally acting oximes in reactivation of tabun-phosphoramidated AChE

Z Kovarik, N Maček, RK Sit, Z Radić, VV Fokin… - Chemico-biological …, 2013 - Elsevier
Organophosphates (OP) inhibit acetylcholinesterase (AChE, EC 3.1. 1.7), both in peripheral
tissues and central nervous system (CNS), causing adverse and sometimes fatal effects due …

Butyrylcholinesterase inhibited by nerve agents is efficiently reactivated with chlorinated pyridinium oximes

T Zorbaz, D Malinak, K Kuca, K Musilek… - Chemico-biological …, 2019 - Elsevier
Bispyridinium oximes with one (K865, K866, K867) or two (K868, K869, K870) ortho-
positioned chlorine moiety, analogous to previously known K027, K048 and K203 oximes …