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Abstract
Acetylcholinesterase reactivators are crucial antidotes for the treatment of organophosphate intoxication. Among the organophosphates, with the exception of soman, tabun (GA) intoxications are the least responsive to treatment with commercially available therapeutics. A rational design was used to increase reactivation ability and decrease the toxicity of the novel reactivator. (E)-1-(4-carbamoylpyridinium)-4-(4-hydroxyiminomethylpyridinium)-but-2-ene dibromide (K203) has better properties than previously tested compounds in vitro and, therefore, is a potential candidate for the treatment of GA intoxication in vivo.
Original language | English |
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Pages (from-to) | 5514-5518 |
Number of pages | 5 |
Journal | Journal of Medicinal Chemistry |
Volume | 50 |
DOIs | |
Publication status | Published - 1 Nov 2007 |
Keywords
- BISPYRIDINIUM COMPOUNDS BEARING
- ACETYLCHOLINESTERASE REACTIVATORS
- CHOLINESTERASE REACTIVATORS
- CRYSTAL-STRUCTURES
- OXIMES
- AGENT
- OBIDOXIME
- TOXICITY
- LINKER
- SERIES
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Dive into the research topics of 'Design of a Potent Reactivator of Tabun-Inhibited Acetylcholinesterase - Synthesis and evaluation of (E)-1-(4-carbamoylpyridinium)-4-(4-hydroxyiminomethylpyridinium)-but-2-ene Dibromide (K203)'. Together they form a unique fingerprint.Projects
- 1 Finished
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MRC G400930: Novel markers for the early detection of Alzheimer's disease
Gunn-Moore, F. J. (PI)
1/07/05 → 31/12/07
Project: Standard