Results 51 to 60 of about 687 (168)

Aminoalkoxy‐substituted coumarins: Synthesis and evaluation for reactivation of inhibited human acetylcholinesterase

Archiv der Pharmazie, Volume 355, Issue 11, November 2022., 2022
Significant effort has been invested into the development of cholinesterase reactivators that are capable of treating organophosphorus poisoning. A series of 12 coumarin derivatives equipped with linker‐connected nonaromatic terminal amino moieties were prepared in this study.
Paul W. Elsinghorst, Timo Wille, Danijela Barić, Matthias D. Mertens, Madlen Baumann, Jim Küppers, Michael Gütschow   +6 more
wiley   +1 more source

1,3–Bis(2–hydroxyiminomethylpyridinium) Propane as the Potential Reactivator of the Acetylcholinesterase Inhibited by Nerve Agents

Acta Medica, 2004
The oxime K005 [1,3–bis(2–hydroxyiminomethylpyridinium) propane dibromide] for the reactivation of the enzyme acetylcholinesterase (AChE) inhibited by cyclosarin and VX was tested.
Kamil Kuča, Vlastimil Dohnal
doaj   +1 more source

Synthesis of Deuterated Methylphosphonic Acid Derivatives for Use as Standard Compounds in the Analysis of Toxic Chemicals

Вестник войск РХБ защиты, 2021
One of the ways to ensure high reliability of detection, identification and accuracy of quantitative determination of toxic chemicals (TC) in environmental and biomedical samples by gas and liquid chromatography-mass spectrometry methods is to use ...
V. А. Yashkir, V. I. Krylov, I. I. Krylov, A. V. Brown, D. V. Oreshkin, I. V. Rybalchenko, V. N. Fateenkov   +6 more
doaj   +1 more source

Human Carboxylesterase 1 Stereoselectively Binds the Nerve Agent Cyclosarin and Spontaneously Hydrolyzes the Nerve Agent Sarin [PDF]

, 2009
Organophosphorus (OP) nerve agents are potent toxins that inhibit cholinesterases and produce a rapid and lethal cholin-ergic crisis. Development of protein-based therapeutics is be-ing pursued with the goal of preventing nerve agent toxicity and ...
Monika Wierdl, Mary Macdonald, Tamara C. Otto, Matthew R. Redinbo, Fleming, C. D., Hemmert, A. C., Douglas M. Cerasoli, MacDonald, M., Cashman, J. R., Christopher D. Fleming, Edwards, C. C., Carol C. Edwards, Andrew C. Hemmert, Wierdl, M., Potter, P. M., Philip M. Potter, Redinbo, M. R., John R. Cashman, Otto, T. C., Cerasoli, D. M.   +19 more
core   +1 more source

Nerve agent hydrolysis activity designed into a human drug metabolism enzyme. [PDF]

PLoS ONE, 2011
Organophosphorus (OP) nerve agents are potent suicide inhibitors of the essential neurotransmitter-regulating enzyme acetylcholinesterase. Due to their acute toxicity, there is significant interest in developing effective countermeasures to OP poisoning.
Andrew C Hemmert, Tamara C Otto, Roberto A Chica, Monika Wierdl, Jonathan S Edwards, Steven M Lewis, Carol C Edwards, Lyudmila Tsurkan, C Linn Cadieux, Shane A Kasten, John R Cashman, Stephen L Mayo, Philip M Potter, Douglas M Cerasoli, Matthew R Redinbo   +14 more
doaj   +1 more source

Evaluation of high-affinity phenyltetrahydroisoquinoline aldoximes, linked through anti-triazoles, as reactivators of phosphylated cholinesterases. [PDF]

Toxicol Lett, 2020
Acetylcholinesterase (AChE) is a pivotal enzyme in neurotransmission. Its inhibition leads to cholinergic crises and could ultimately result in death.
Maček Hrvat N, Kalisiak J, Šinko G, Radić Z, Sharpless KB, Taylor P, Kovarik Z.   +6 more
europepmc   +2 more sources

Potency of new structurally different oximes to reactivate cyclosarin-inhibited human brain acetylcholinesterases [PDF]

Journal of Enzyme Inhibition and Medicinal Chemistry, 2006
Antidotes currently used for organophosphorus pesticide and nerve agent intoxications consist of anticholinergics (atropine mainly) and acetylcholinesterase (AChE, EC 3.1.1.7) reactivators called oximes. Owing to the wide-spread of these toxic compounds worldwide, development of antidotes in the case of first aid is needed. To select the most promising
Kamil, Kuca, Jiri, Cabal, Daniel, Jun, Jiri, Bajgar, Martina, Hrabinova   +4 more
openaire   +2 more sources

Bimolecular rates of inhibition, Michaelis-Menten constants, and rates of reactivation for wild-type and V146H/L363E hCE1 against racemic cyclosarin and stereoisomers of cyclosarin model compounds.

, 2013
N = 3, s.d., N.D. is not determined, N.R. is no reactivation, pH 7.4, 25°C.aRacemic bona fide cyclosarin,bstereoisomers of cyclosarin model compounds,c(8).
Steven L. Lewis (354519), Matthew R. Redinbo (93591), Carol C. Edwards (354521), Tamara C. Otto (350617), Philip M. Potter (23125), Douglas M. Cerasoli (350618), C. Linn Cadieux (354524), John R. Cashman (354526), Lyudmila Tsurkan (354523), Shane A. Kasten (354525), Roberto A. Chica (109101), Stephen L. Mayo (109096), Monika Wierdl (354512), Jonathan S. Edwards (354516), Andrew C. Hemmert (354510)   +14 more
core   +1 more source

In vitro detoxification of cyclosarin in human blood pre-incubated ex vivo with recombinant serum paraoxonases [PDF]

Toxicology Letters, 2011
An ex vivo protocol was developed to assay the antidotal capacity of rePON1 variants to protect endogenous acetylcholinesterase and butyrylcholinesterase in human whole blood against OP nerve agents. This protocol permitted us to address the relationship between blood rePON1 concentrations, their kinetic parameters, and the level of protection ...
Yacov, Ashani, Moshe, Goldsmith, Haim, Leader, Israel, Silman, Joel L, Sussman, Dan S, Tawfik   +5 more
openaire   +2 more sources

Mechanism of reactivation by V146H/L363E hCE1 after cyclosarin binding.

, 2013
A. Model of V146H/L363E (cyan) hCE1 with PR cyclosarin (magenta) including a water molecule (red) between E363 and the central phosphorus. B. Proposed mechanism for enhanced reactivation following cyclosarin inhibition. C.
Steven L. Lewis (354519), Matthew R. Redinbo (93591), Carol C. Edwards (354521), Tamara C. Otto (350617), Philip M. Potter (23125), Douglas M. Cerasoli (350618), C. Linn Cadieux (354524), John R. Cashman (354526), Lyudmila Tsurkan (354523), Shane A. Kasten (354525), Roberto A. Chica (109101), Stephen L. Mayo (109096), Monika Wierdl (354512), Jonathan S. Edwards (354516), Andrew C. Hemmert (354510)   +14 more
core   +1 more source