Quaternary salts of E2020 analogues as acetylcholinesterase inhibitors for the reversal of neuromuscular block.
A series benzylpiperidinium and benzylpyridinium quaternary salts have been synthesised and tested for inhibition of acetylcholinesterase and reversal of neuromuscular block induced by vecuronium. Several potent reversal agents have been identified and their haemodynamic effects measured.
Department of Medicinal Chemistry, Organon Laboratories Ltd., Newhouse, Lanarkshire ML1 5SH, UK. jk.clark@organon@co.uk
John K
JK
Clark
Phill
P
Cowley
Alan W
AW
Muir
Ronald
R
Palin
Eleanor
E
Pow
Alan B
AB
Prosser
Robert
R
Taylor
Ming-Qiang
MQ
Zhang
D000110:Acetylcholinesterase / Q000187:drug effects*; D002800:Cholinesterase Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D000077265:Donepezil; D007189:Indans / Q000737:chemistry / Q000494:pharmacology*; D003473:Neuromuscular Nondepolarizing Agents / Q000037:antagonists & inhibitors*; D010880:Piperidines / Q000737:chemistry / Q000494:pharmacology*; D014673:Vecuronium Bromide / Q000037:antagonists & inhibitors*
D002800:Cholinesterase Inhibitors; D007189:Indans; D003473:Neuromuscular Nondepolarizing Agents; D010880:Piperidines; D014673:Vecuronium Bromide; D000077265:Donepezil; D000110:Acetylcholinesterase