Strategies for enhanced bioavailability of oxime reactivators in the central nervous system

E Prchalova, Z Kohoutova, K Knittelova, D Malinak… - Archives of …, 2023 - Springer
Oxime reactivators of acetylcholinesterase are commonly used to treat highly toxic
organophosphate poisoning. They are effective nucleophiles that can restore the catalytic …

The risk associated with organophosphorus nerve agents: from their discovery to their unavoidable threat, current medical countermeasures and perspectives

C Voros, J Dias, CM Timperley, F Nachon… - Chemico-biological …, 2024 - Elsevier
The first organophosphorus nerve agent was discovered accidently during the development
of pesticides, shortly after the first use of chemical weapons (chlorine, phosgene) on the …

Cholesterol oxime olesoxime assessed as a potential ligand of human cholinesterases

D Kolić, G Šinko, L Jean, M Chioua, J Dias… - Biomolecules, 2024 - mdpi.com
Olesoxime, a cholesterol derivative with an oxime group, possesses the ability to cross the
blood–brain barrier, and has demonstrated excellent safety and tolerability properties in …

Brominated oxime nucleophiles are efficiently reactivating cholinesterases inhibited by nerve agents

E Prchalova, R Andrys, J Pejchal, Z Kohoutova… - Archives of …, 2024 - Springer
Six novel brominated bis-pyridinium oximes were designed and synthesized to increase
their nucleophilicity and reactivation ability of phosphorylated acetylcholinesterase (AChE) …

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

M Mlakić, T Čadež, G Šinko, I Škorić, Z Kovarik - Biomolecules, 2024 - mdpi.com
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) …

Reactivators of butyrylcholinesterase inhibited by organophosphorus compounds

Z Kohoutova, E Prchalova, K Knittelova, K Musilek… - Bioorganic …, 2024 - Elsevier
In this review, the current progress in the research and development of butyrylcholinesterase
(BChE) reactivators is summarised and the advantages or disadvantages of these …

Dysregulation of butyrylcholinesterase, BCHE gene SNP rs1803274, and pro-inflammatory cytokines in occupational workers

SA Khan, MNL Javeres, STA Shah, N Bibi… - Environmental …, 2023 - Elsevier
Background. People in different occupations are exposed to a variety of xenobiotics which
affect the health and physiological processes of the body. Butyrylcholinesterase (BChE), has …

[HTML][HTML] Potential of vitamin B6 dioxime analogues to act as cholinesterase ligands

D Gašo Sokač, A Zandona, S Roca… - International journal of …, 2022 - mdpi.com
Seven pyridoxal dioxime quaternary salts (1–7) were synthesized with the aim of studying
their interactions with human acetylcholinesterase (AChE) and butyrylcholinesterase …

[PDF][PDF] FLUORINATED AND CHLORINATED PYRIDINIUM OXIMES REACTIVATING CHOLINESTERASES INHIBITED BY NERVE AGENTS

D Malinak, T Zorbaz, T Hofmanova, R Andrys, M Psotka… - mmsl.cz
Nerve agents are organophosphorus compounds (OPs) with very potent toxicity due to their
irreversible inhibition of the essential enzymeacetylcholinesterase (AChE; EC 3.1. 1.7) …

NERVE AGENT INHIBITED CHOLINESTERASES CAN BE EFFICIENTLY REACTIVATED BY OXIMES WITH ENHANCED NUCLEOPHILICITY

K Musilek, D Malinak, T Zorbaz, R Andrys, Z Kohoutova… - mmsl.cz
Organophosphorus compounds (eg nerve agents-sarin, VX or tabun) cause deleterious
intoxications via inhibition of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) …