Novel water soluble 2,6-dimethoxyphenyl ester derivatives with intravenous anaesthetic activity.
A number of water soluble bis-amino-2,6-dimethoxyphenyl ester derivatives were found to exhibit improved anaesthetic activity in mice relative to propofol 1. Of the analogues disclosed, 44 was further profiled in rodents and found to be a superior agent to propofol for the induction and maintenance of anaesthesia.
Bennett
D Jonathan
DJ
Departments of Medicinal Chemistry and Pharmacology, Organon Laboratories Ltd., Newhouse, Motherwell ML1 5SH, Scotland, UK. j.bennett@organon.co.uk
Anderson
Alison
A
Buchanan
Kirsteen
K
Byford
Alan
A
Cooke
Andrew
A
Gemmell
David K
DK
Hamilton
Niall M
NM
Maidment
Maurice S
MS
McPhail
Petula
P
Stevenson
Donald F M
DF
Sundaram
Hardy
H
Vijn
Peter
P
D018686:Anesthetics, Intravenous / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D000818:Animals; D019086:Bridged Bicyclo Compounds, Heterocyclic / Q000378:metabolism; D004569:Electroencephalography / Q000187:drug effects; D004952:Esters / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D007262:Infusions, Intravenous / Q000379:methods; D008297:Male; D051379:Mice; D008817:Mice, Mutant Strains; D010636:Phenols / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D015742:Propofol / Q000494:pharmacology; D051381:Rats; D017208:Rats, Wistar; D011963:Receptors, GABA-A / Q000187:drug effects; D012995:Solubility; D013329:Structure-Activity Relationship; D014867:Water / Q000737:chemistry
D018686:Anesthetics, Intravenous; D019086:Bridged Bicyclo Compounds, Heterocyclic; D004952:Esters; D010636:Phenols; D011963:Receptors, GABA-A; D014867:Water; C037476:tert-butylbicyclophosphorothionate; D015742:Propofol