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 …

Review about structure and evaluation of reactivators of Acetylcholinesterase inhibited with neurotoxic organophosphorus compounds

JD Figueroa-Villar, EC Petronilho… - Current medicinal …, 2021 - ingentaconnect.com
Background: Neurotoxic chemical warfare agents can be classified as some of the most
dangerous chemicals for humanity. The most effective of those agents are the …

Oximes: inhibitors of human recombinant acetylcholinesterase. A structure-activity relationship (SAR) study

V Sepsova, JZ Karasova, J Korabecny… - International journal of …, 2013 - mdpi.com
Acetylcholinesterase (AChE) reactivators were developed for the treatment of
organophosphate intoxication. Standard care involves the use of anticonvulsants (eg …

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 …

Monooxime‐monocarbamoyl bispyridinium xylene‐linked reactivators of acetylcholinesterase—synthesis, in vitro and toxicity evaluation, and docking studies

K Musilek, O Holas, J Misik, M Pohanka… - ChemMedChem …, 2010 - Wiley Online Library
Acetylcholinesterase (AChE) reactivators are crucial antidotes to organophosphate
intoxication. A new series of 26 monooxime‐monocarbamoyl xylene‐linked bispyridinium …

Monooxime reactivators of acetylcholinesterase with (E)-but-2-ene linker—Preparation and reactivation of tabun-and paraoxon-inhibited acetylcholinesterase

K Musilek, O Holas, D Jun, V Dohnal… - Bioorganic & medicinal …, 2007 - Elsevier
Acetylcholinesterase reactivators are crucial antidotes for the treatment of organophosphate
intoxication. Fifteen new monooxime reactivators of acetylcholinesterase with a (E)-but-2 …

Novel series of bispyridinium compounds bearing a (Z)-but-2-ene linker—Synthesis and evaluation of their reactivation activity against tabun and paraoxon-inhibited …

K Musilek, O Holas, K Kuca, D Jun, V Dohnal… - Bioorganic & medicinal …, 2007 - Elsevier
Six novel AChE reactivators with a (Z)-but-2-ene linker were synthesized using the known
synthetic pathways. Their ability to reactivate AChE, which had been previously inhibited by …

[PDF][PDF] Could oxime HI-6 really be considered as “broad-spectrum” antidote

K Kuča, K Musílek, D Jun, M Pohanka… - J appl …, 2009 - academia.edu
The broad-spectrum reactivator is a valuable oxime able to reactivate acetylcholinesterase
(AChE) inhibited by nerve agents and pesticides. At present there are many AChE …

Monoquaternary pyridinium salts with modified side chain—synthesis and evaluation on model of tabun-and paraoxon-inhibited acetylcholinesterase

K Musilek, J Kucera, D Jun, V Dohnal… - Bioorganic & medicinal …, 2008 - Elsevier
Acetylcholinesterase reactivators are crucial antidotes for the treatment of organophosphate
intoxication. Eighteen monoquaternary reactivators of acetylcholinesterase with modified …

The development of new oximes and the evaluation of their reactivating, therapeutic and neuroprotective efficacy against tabun

J Kassa, K Kuca, J Karasova… - Mini reviews in medicinal …, 2008 - ingentaconnect.com
Tabun (O-ethyl-N, N-dimethyl phosphoramidocyanidate) belongs to highly toxic
organophosphorus compounds misused as chemical warfare agents for military as well as …