Oxyaniliniums as acetylcholinesterase inhibitors for the reversal of neuromuscular block.
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.
Grove
Simon J A
SJ
Department of Medicinal Chemistry, Organon Laboratories Ltd., Newhouse, Lanarkshire ML1 5SH, Scotland, UK.
Kaur
Jasmit
J
Muir
Alan W
AW
Pow
Eleanor
E
Tarver
Gary J
GJ
Zhang
Ming-Qiang
MQ
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
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