Development and Structural Modifications of Cholinesterase Reactivators against Chemical Warfare Agents in Last Decade: A Review.

摘要: Organophosphate (OP) pesticides and nerve agents are responsible for suicidal accidental poisonings. The acute toxicity of leads to progressive inhibition the enzyme acetylcholinesterase (AChE) by phosphylation of serine residue at active site gorge. The recent massive destruction Syrian civilians gas sarin, has again renewed research attention global science fraternity towards agents, their mode action most prominently therapeutic treatment. This review is principally focused on agent intoxication. common approach deal with OP-intoxication is, application antimuscarinic drug (atropine), anticonvulsant (diazepam) and clinically used oximes (pralidoxime, trimedoxime, obidoxime asoxime). However, existing therapeutic approach arguable has several failings cure all kinds Considering this issue, numerous oximes have been synthesized screened through various in-vitro in-vivo studies in last decade overcome the downsides. At present, only a few (bis pyridinum-oximes) exhibit sound efficacy against selective OPs. In spite of extensive efforts, till date no oxime available as universal antidote classes is centered developments structural modification AChE reactivators toxicity. In particular, deeper look taken into chemical modifications incorporation different structural moieties targeted increased reactivation affinity improved blood brain barrier (BBB) penetration.