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- W2096430284 endingPage "72" @default.
- W2096430284 startingPage "58" @default.
- W2096430284 abstract "Organophosphate (OP) pesticides and nerve agents are responsible for suicidal and accidental poisonings. The acute toxicity of nerve agents leads to progressive inhibition of the enzyme acetylcholinesterase (AChE) by phosphylation of serine residue at the active site of gorge. The recent massive destruction of Syrian civilians by nerve gas sarin, has again renewed the research attention of global science fraternity towards nerve agents, their mode of action and most prominently their therapeutic treatment. This review is principally focused on nerve agent intoxication. The common approach to deal with OP-intoxication is, application of antimuscarinic drug (atropine), anticonvulsant drug (diazepam) and clinically used oximes (pralidoxime, trimedoxime, obidoxime and asoxime). However, the existing therapeutic approach is arguable and has several failings to cure all kinds of nerve agent poisonings. Considering this issue, numerous oximes have been synthesized and screened through various in-vitro and in-vivo studies in last decade to overcome the downsides. At present, only a few oximes (bis pyridinum-oximes) exhibit sound efficacy against selective OPs. In spite of extensive efforts, till date no oxime is available as a universal antidote against all the classes of OPs. This review is centered on the recent developments and structural modification of AChE reactivators against nerve agent toxicity. In particular, a deeper look has been taken into chemical modifications of the reactivators by incorporation of different structural moieties targeted towards the increased reactivation affinity and improved blood brain barrier (BBB) penetration. Keywords: AChE, BBB, chemical warfare agents, organophosphates, oxime, reactivator." @default.
- W2096430284 created "2016-06-24" @default.
- W2096430284 creator A5020861227 @default.
- W2096430284 creator A5041445236 @default.
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- W2096430284 creator A5055182438 @default.
- W2096430284 creator A5066903927 @default.
- W2096430284 creator A5081044946 @default.
- W2096430284 date "2015-02-24" @default.
- W2096430284 modified "2023-10-14" @default.
- W2096430284 title "Development and Structural Modifications of Cholinesterase Reactivators against Chemical Warfare Agents in Last Decade: A Review" @default.
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