title: Novel bisquaternary oximes--reactivation of acetylcholinesterase and butyrylcholinesterase inhibited by paraoxon.
abstract: Four novel bisquaternary aldoxime cholinesterase reactivators differing in their chemical structure were prepared. Afterwards, their biological activity was evaluated for their ability to reactivate acetylcholinesterase (AChE; EC 3.1.1.7) and butyrylcholinesterase (BuChE; EC 3.1.1.8) inhibited by paraoxon. Their reactivation activity was compared with standard reactivators--pralidoxime, obidoxime and HI-6--which are clinically used at present. As it resulted, none of the prepared compounds surpassed obidoxime, which is considered to be the most potent compound if used for reactivation of AChE inhibited by paraoxon. In case of BuChE reactivation, two compounds (K053 and K068) achieved similar results as obidoxime.
authors.affiliation: Faculty of Military Health Sciences, University of Defence, Hradec Kralove, Czech Republic. kucakam@pmfhk.cz
authors.forename: Kamil
authors.initials: K
authors.lastname: Kuca
authors.forename: Lucie
authors.initials: L
authors.lastname: Musilova
authors.forename: Jiri
authors.initials: J
authors.lastname: Palecek
authors.forename: Vladimir
authors.initials: V
authors.lastname: Cirkva
authors.forename: Martin
authors.initials: M
authors.lastname: Paar
authors.forename: Kamil
authors.initials: K
authors.lastname: Musilek
authors.forename: Martina
authors.initials: M
authors.lastname: Hrabinova
authors.forename: Miroslav
authors.initials: M
authors.lastname: Pohanka
authors.forename: Jana Zdarova
authors.initials: JZ
authors.lastname: Karasova
authors.forename: Daniel
authors.initials: D
authors.lastname: Jun
mesh_terms: D000110:Acetylcholinesterase / Q000187:drug effects* / Q000378:metabolism; D002091:Butyrylcholinesterase / Q000187:drug effects* / Q000378:metabolism; D004793:Enzyme Reactivators / Q000494:pharmacology*; D009682:Magnetic Resonance Spectroscopy; D010091:Oximes / Q000737:chemistry*; D010261:Paraoxon / Q000494:pharmacology*
chemical_list: D004793:Enzyme Reactivators; D010091:Oximes; D000110:Acetylcholinesterase; D002091:Butyrylcholinesterase; D010261:Paraoxon