Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1377251 | Bioorganic & Medicinal Chemistry Letters | 2006 | 4 Pages |
Abstract
The preparation of the sulfoxide analogues 7, 8, and 9 and their enantiomerically pure forms is discussed as well as their ability to act as prodrugs of the potent and selective sulfone-containing COX-2 inhibitors 1, 2, and 3. Sulfoxide derivatives 7 and 9 were shown to be rapidly transformed in vivo into the corresponding sulfone derivatives 1 and 3, after oral administration to rats.
Graphical abstractThe enantiomeric synthesis and profiling of sulfoxide-based prodrugs of potent COX-2 inhibitors discovered at Almirall are reported.Figure optionsDownload full-size imageDownload as PowerPoint slide
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Francisco Caturla, Mercè Amat, Raquel F. Reinoso, Elena Calaf, Graham Warrellow,