Oxyaniliniums as acetylcholinesterase inhibitors for the reversal of neuromuscular block

Bioorg Med Chem Lett. 2002 Jan 21;12(2):193-6. doi: 10.1016/s0960-894x(01)00703-x.

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