Water-soluble propofol analogues with intravenous anaesthetic activity.
Propofol (2,6-diisopropylphenol) is a widely used intravenous anaesthetic that is formulated as an emulsion since it lacks water solubility. We report a range of water-soluble analogues of propofol, containing a para-alkylamino substituent, which retain good intravenous anaesthetic activity in rodents.
Cooke
A
A
Department of Medicinal Chemistry and Pharmacology, Organon Laboratories Ltd., Newhouse, Scotland, UK. a.cooke@organon.nhe.akzonobel.nl
Anderson
A
A
Buchanan
K
K
Byford
A
A
Gemmell
D
D
Hamilton
N
N
McPhail
P
P
Miller
S
S
Sundaram
H
H
Vijn
P
P
D018686:Anesthetics, Intravenous / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D000814:Aniline Compounds / Q000737:chemistry*; D000818:Animals; D004569:Electroencephalography / Q000187:drug effects; D020128:Inhibitory Concentration 50; D008297:Male; D051379:Mice; D015742:Propofol / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology*; D051381:Rats; D017208:Rats, Wistar; D011963:Receptors, GABA-A / Q000187:drug effects*; D012995:Solubility; D013329:Structure-Activity Relationship
D018686:Anesthetics, Intravenous; D000814:Aniline Compounds; D011963:Receptors, GABA-A; C023650:aniline; D015742:Propofol