title: Oxyaniliniums as acetylcholinesterase inhibitors for the reversal of neuromuscular block.
abstract: A series of oxyanilinium-based AChE inhibitors have been synthesised and tested for the reversal of vecuronium-induced neuromuscular block. Several compounds, for example 2-hydroxy- and 2-methoxy-N,N-dimethyl-N-allylanilinium bromide (3 and 6) showed comparable reversal potencies to edrophonium and clean in vivo cardiovascular profiles.
authors.affiliation: Department of Medicinal Chemistry, Organon Laboratories Ltd., Newhouse, Lanarkshire ML1 5SH, Scotland, UK.
authors.forename: Simon J A
authors.initials: SJ
authors.lastname: Grove
authors.forename: Jasmit
authors.initials: J
authors.lastname: Kaur
authors.forename: Alan W
authors.initials: AW
authors.lastname: Muir
authors.forename: Eleanor
authors.initials: E
authors.lastname: Pow
authors.forename: Gary J
authors.initials: GJ
authors.lastname: Tarver
authors.forename: Ming-Qiang
authors.initials: MQ
authors.lastname: Zhang
mesh_terms: D000110:Acetylcholinesterase / Q000187:drug effects*; D000498:Allyl Compounds / Q000737:chemistry / Q000494:pharmacology*; D000814:Aniline Compounds / Q000737:chemistry / Q000494:pharmacology*; D002800:Cholinesterase Inhibitors / Q000494:pharmacology*; D018360:Crystallography, X-Ray; D004491:Edrophonium / Q000037:antagonists & inhibitors*; D009466:Neuromuscular Blocking Agents / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship
chemical_list: C449667:2-hydroxy-N,N-dimethyl-N-allylanilinium bromide; C449668:2-methoxy-N,N-dimethyl-N-allylanilinium bromide; D000498:Allyl Compounds; D000814:Aniline Compounds; D002800:Cholinesterase Inhibitors; D009466:Neuromuscular Blocking Agents; D004491:Edrophonium; D000110:Acetylcholinesterase