PMID: 16515465Mar 7, 2006Paper

Structural requirements of acetylcholinesterase reactivators

Mini Reviews in Medicinal Chemistry
Kamil KucaKamil Musilek

Abstract

Nerve agents (sarin, soman, cyclosarin, tabun and VX agent) and pesticides (paraoxon, chlorpyrifos, TEPP) represent extremely toxic group of organophosphorus compounds (OPCs). These compounds inhibit enzyme acetylcholinesterase (AChE, EC 3.1.1.7) via its phosphorylation or phosphonylation at the serine hydroxy group in its active site. Afterwards, AChE is not able to serve its physiological function and intoxicated organism is died due to overstimulation of cholinergic nervous system. The current standard treatment of poisoning with highly toxic OPCs usually consists of the combined administration of anticholinergic drugs (preferably atropine) and AChE reactivators (called "oximes"). Anticholinergic drugs block effects of accumulated neurotransmitter acetylcholine at nicotinic and muscarinic receptor sites, while oximes reactivate AChE inhibited by OPCs. Unfortunately, none from the currently used oximes is sufficiently effective against all known nerve agents and pesticides. Therefore, to find new oximes able to sufficiently reactivate inhibited AChE (regardless of the type of OPCs) is still very important task for medicinal chemistry with the aim to improve the efficacy of antidotal treatment of the acute poisonings mentioned...Continue Reading

Citations

Jun 15, 2011·Chemical Reviews·Kibong KimDavid G Churchill
Mar 29, 2011·Journal of Medicinal Chemistry·Jarosław KalisiakJohn R Cashman
Jan 12, 2007·The Neurologist·Jonathan Newmark
Sep 11, 2009·International Journal of Molecular Sciences·Jana Zdarova KarasovaKamil Kuca
Mar 31, 2009·International Journal of Molecular Sciences·Jana Zdarova KarasovaKamil Kuca
Apr 23, 2013·Pharmacology & Therapeutics·Franz Worek, Horst Thiermann
Jan 27, 2007·Journal of Enzyme Inhibition and Medicinal Chemistry·Kamil KucaMartina Hrabinova
Oct 1, 2008·Journal of Enzyme Inhibition and Medicinal Chemistry·Miroslav PohankaKamil Kuca
Dec 30, 2006·Journal of Enzyme Inhibition and Medicinal Chemistry·Martina HrabinovaKamil Kuca
Jul 11, 2008·Journal of Enzyme Inhibition and Medicinal Chemistry·Miroslav PohankaKamil Kuca
Jul 10, 2009·Clinical Toxicology : the Official Journal of the American Academy of Clinical Toxicology and European Association of Poisons Centres and Clinical Toxicologists·Lucie MusilovaDaniel Jun
Dec 29, 2007·Drug and Chemical Toxicology·Daniel JunJan Marek
May 16, 2007·Clinical Toxicology : the Official Journal of the American Academy of Clinical Toxicology and European Association of Poisons Centres and Clinical Toxicologists·Kamil KucaMartina Hrabinova
Aug 8, 2008·Clinical Toxicology : the Official Journal of the American Academy of Clinical Toxicology and European Association of Poisons Centres and Clinical Toxicologists·Jiri KassaJiri Bajgar
Dec 15, 2015·Chemical Reviews·Yoon Jeong JangDavid G Churchill
Aug 7, 2010·Toxicology in Vitro : an International Journal Published in Association with BIBRA·Jyotiranjan AcharyaSyed Kalbey Raza
Jul 6, 2010·Toxicology in Vitro : an International Journal Published in Association with BIBRA·Jyotiranjan AcharyaSyed Kalbey Raza
Jul 27, 2011·Environmental Toxicology and Pharmacology·Kamil KucaYoung-Sik Jung
May 1, 2008·Environmental Toxicology and Pharmacology·Sarka VeselaDaniel Jun
May 29, 2009·Basic & Clinical Pharmacology & Toxicology·Kamil KucaMartina Hrabinova
Jun 20, 2007·Basic & Clinical Pharmacology & Toxicology·Kamil KucaLucie Musilova

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