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...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2002-01, Vol.12 (2), p.193-196
Hauptverfasser:	Grove, Simon J.A., Kaur, Jasmit, Muir, Alan W., Pow, Eleanor, Tarver, Gary J., Zhang, Ming-Qiang
Format:	Artikel
Sprache:	eng
Schlagworte:	Acetylcholinesterase - drug effects Allyl Compounds - chemistry Allyl Compounds - pharmacology Aniline Compounds - chemistry Aniline Compounds - pharmacology Biological and medical sciences Cholinergic system Cholinesterase Inhibitors - pharmacology Crystallography, X-Ray Edrophonium - antagonists & inhibitors Medical sciences Neuromuscular Blocking Agents - antagonists & inhibitors Neuropharmacology Neurotransmitters. Neurotransmission. Receptors Pharmacology. Drug treatments Structure-Activity Relationship
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Zusammenfassung:	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. Graphic
ISSN:	0960-894X 1464-3405
DOI:	10.1016/S0960-894X(01)00703-X