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.
MeSH terms
-
Acetylcholinesterase / drug effects*
-
Allyl Compounds / chemistry
-
Allyl Compounds / pharmacology*
-
Aniline Compounds / chemistry
-
Aniline Compounds / pharmacology*
-
Cholinesterase Inhibitors / pharmacology*
-
Crystallography, X-Ray
-
Edrophonium / antagonists & inhibitors*
-
Neuromuscular Blocking Agents / antagonists & inhibitors*
-
Structure-Activity Relationship
Substances
-
2-hydroxy-N,N-dimethyl-N-allylanilinium bromide
-
2-methoxy-N,N-dimethyl-N-allylanilinium bromide
-
Allyl Compounds
-
Aniline Compounds
-
Cholinesterase Inhibitors
-
Neuromuscular Blocking Agents
-
Edrophonium
-
Acetylcholinesterase