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)

K Musilek, D Jun, J Cabal, J Kassa, Francis James Gunn-Moore, K Kuca

Research output: Contribution to journalArticlepeer-review

102 Citations (Scopus)

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 languageEnglish
Pages (from-to)5514-5518
Number of pages5
JournalJournal of Medicinal Chemistry
Volume50
DOIs
Publication statusPublished - 1 Nov 2007

Keywords

  • BISPYRIDINIUM COMPOUNDS BEARING
  • ACETYLCHOLINESTERASE REACTIVATORS
  • CHOLINESTERASE REACTIVATORS
  • CRYSTAL-STRUCTURES
  • OXIMES
  • AGENT
  • OBIDOXIME
  • TOXICITY
  • LINKER
  • SERIES

Fingerprint

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.

Cite this