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 …

Recent developments on oximes to improve the blood brain barrier penetration for the treatment of organophosphorus poisoning: a review

MNF Norrrahim, MAIA Razak, NAA Shah, H Kasim… - RSC …, 2020 - pubs.rsc.org
Organophosphorus (OP) compounds are highly toxic synthetic compounds which have been
used as pesticides and developed as warfare nerve agents. They represent a threat to both …

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 …

Potent 3‐Hydroxy‐2‐Pyridine Aldoxime Reactivators of Organophosphate‐Inhibited Cholinesterases with Predicted Blood–Brain Barrier Penetration

T Zorbaz, A Braïki, N Maraković… - … A European Journal, 2018 - Wiley Online Library
A new series of 3‐hydroxy‐2‐pyridine aldoxime compounds have been designed,
synthesised and tested in vitro, in silico, and ex vivo as reactivators of human …

A comprehensive evaluation of the efficacy of leading oxime therapies in guinea pigs exposed to organophosphorus chemical warfare agents or pesticides

CM Wilhelm, TH Snider, MC Babin, DA Jett… - Toxicology and applied …, 2014 - Elsevier
The currently fielded pre-hospital therapeutic regimen for the treatment of
organophosphorus (OP) poisoning in the United States (US) is the administration of atropine …

Evaluation of oxime K203 as antidote in tabun poisoning

Z Kovarik, A Lucić Vrdoljak, S Berend… - Arhiv za higijenu rada i …, 2009 - hrcak.srce.hr
Sažetak We studied bispyridinium oxime K203 [(E)-1-(4-carbamoylpyridinium)-4-(4-
hydroxyimino methylpyridinium)-but-2-ene dibromide] with tabun-inhibited human …

Comparative protective effects of HI-6 and MMB-4 against organophosphorous nerve agent poisoning

PM Lundy, MG Hamilton, TW Sawyer, J Mikler - Toxicology, 2011 - Elsevier
Abstract The oximes pralidoxime (2-PAM), its dimethanesulphonate salt derivative P2S, and
obidoxime (toxogonin) are currently licensed and fielded for the treatment of chemical …

Reversal of Tabun Toxicity Enabled by a Triazole‐Annulated Oxime Library—Reactivators of Acetylcholinesterase

Z Kovarik, J Kalisiak, NM Hrvat… - … A European Journal, 2019 - Wiley Online Library
Acetylcholinesterase (AChE), an enzyme that degrades the neurotransmitter acetylcholine,
when covalently inhibited by organophosphorus compounds (OPs), such as nerve agents …

Design and synthesis of N-substituted-2-hydroxyiminoacetamides and interactions with cholinesterases

N Maraković, A Knežević, V Vinković, Z Kovarik… - Chemico-biological …, 2016 - Elsevier
Within this study, we designed and synthesized four new oxime compounds of the N-
substituted 2-hydroxyiminoacetamide structure and evaluated their interactions with …

The experimental oxime K027—a promising protector from organophosphate pesticide poisoning. A review comparing K027, K048, pralidoxime, and obidoxime

DE Lorke, GA Petroianu - Frontiers in neuroscience, 2019 - frontiersin.org
Poisoning with organophosphorus compounds (OPCs) is a major problem worldwide.
Standard therapy with atropine and established oxime-type enzyme reactivators …