Title of article
Designing rapid onset selective serotonin re-uptake inhibitors. Part 3: Site-directed metabolism as a strategy to avoid active circulating metabolites: Structure–activity relationships of (thioalkyl)phenoxy benzylamines
Author/Authors
Donald S. Middleton، نويسنده , , Mark Andrews، نويسنده , , Paul Glossop، نويسنده , , Geoffrey Gymer، نويسنده , , David Hepworth، نويسنده , , Alan Jessiman، نويسنده , , Patrick S. Johnson، نويسنده , , Malcolm MacKenny، نويسنده , , Alan Stobie، نويسنده , , Kim Tang، نويسنده , , B. Paul Morgan، نويسنده , , Barry Jones، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2008
Pages
4
From page
5303
To page
5306
Abstract
A series of thio-alkyl containing diphenylethers were designed and evaluated, as a strategy to competitively direct metabolism away from unwanted amine N-demethylation and deliver a pharmacologically inactive S-oxide metabolite. Overall, sulfonamide 20 was found to possess the best balance of target pharmacology, pharmacokinetics and metabolism profile.
Keywords
SSRI , Site-directed metabolism , Volume of distribution
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2008
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
800004
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