Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1372688 | Bioorganic & Medicinal Chemistry Letters | 2008 | 4 Pages |
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.
Graphical abstractA 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, sulphonamide 20 was found to possess the best balance of target pharmacology, pharmacokinetics and metabolism profile.Figure optionsDownload full-size imageDownload as PowerPoint slide