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Phenoxypropylamines: A New Series of Squalene Synthase Inhibitors

โœ Scribed by Brown, George R.; Butlin, Roger J.; Chapman, Steven; Eakin, M. Allan; Foubister, Alan J.; Freeman, Susan; Griffiths, David; Harrison, Peter J.; Johnson, Michael C.


Book ID
120607284
Publisher
American Chemical Society
Year
1995
Tongue
English
Weight
493 KB
Volume
38
Category
Article
ISSN
0022-2623

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Novel optimised quinuclidine squalene sy
โœ George R. Brown; Alan J. Foubister; Susan Freeman; Fergus McTaggart; Donald J. M ๐Ÿ“‚ Article ๐Ÿ“… 1997 ๐Ÿ› Elsevier Science ๐ŸŒ English โš– 221 KB

Optimised quinuclidine squalene synthase (SQS) inhibitors are reported; 3-[2-(2-allyl-4-(2-ethoxy carbonylethyl)phenyl)ethynyl]quinuclidin-3-ol lc, is a potent inhibitor of rat (KI = 6 nM) and human (KI = 43 nM) microsomal SQS; the oral EDso of lc, for the inhibition of rat cholesterol biosynthesis