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Bioorg. Med. Chem. Lett. · Sep 2002
Novel piperidinium and pyridinium agents as water-soluble acetylcholinesterase inhibitors for the reversal of neuromuscular blockade.
- Ronald Palin, John K Clark, Phill Cowley, Alan W Muir, Eleanor Pow, Alan B Prosser, Robert Taylor, and Ming-Qiang Zhang.
- Department of Medicinal Chemistry, Organon Laboratories Ltd., Newhouse, Lanarkshire ML1 5SH, UK. r.palin@organon.nhe.akzonobel.nl
- Bioorg. Med. Chem. Lett. 2002 Sep 16;12(18):2569-72.
AbstractA series of piperidinium and pyridinium agents containing a common structural fragment of 5,6-dimethoxybenzothiophene have been synthesised as water-soluble acetylcholinesterase inhibitors. Several compounds, for example 42 (AChE IC(50) 0.03 microM) have been found to reverse the neuromuscular blockade induced by vecuronium bromide in vitro and in vivo. Coupled with their high water solubility (up to 30-60 mg/mL), these compounds are potentially useful as intravenous reversal agents of neuromuscular blocking agents in surgical anaesthesia.
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