Water-soluble propofol analogues with intravenous anaesthetic activity

A Cooke; A Anderson; K Buchanan; A Byford; D Gemmell; N Hamilton; P McPhail; S Miller; H Sundaram; P Vijn

doi:10.1016/s0960-894x(01)00088-9

Water-soluble propofol analogues with intravenous anaesthetic activity

Bioorg Med Chem Lett. 2001 Apr 9;11(7):927-30. doi: 10.1016/s0960-894x(01)00088-9.

Authors

A Cooke¹, A Anderson, K Buchanan, A Byford, D Gemmell, N Hamilton, P McPhail, S Miller, H Sundaram, P Vijn

Affiliation

¹ Department of Medicinal Chemistry and Pharmacology, Organon Laboratories Ltd., Newhouse, Scotland, UK. a.cooke@organon.nhe.akzonobel.nl

PMID: 11294393
DOI: 10.1016/s0960-894x(01)00088-9

Abstract

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.

MeSH terms

Anesthetics, Intravenous / chemical synthesis*
Anesthetics, Intravenous / chemistry
Anesthetics, Intravenous / pharmacology*
Aniline Compounds / chemistry*
Animals
Electroencephalography / drug effects
Inhibitory Concentration 50
Male
Mice
Propofol / analogs & derivatives*
Propofol / chemistry
Propofol / pharmacology*
Rats
Rats, Wistar
Receptors, GABA-A / drug effects*
Solubility
Structure-Activity Relationship

Substances

Anesthetics, Intravenous
Aniline Compounds
Receptors, GABA-A
aniline
Propofol