Racemic and chiral sulfoxides as potential prodrugs of 4-pyrone COX-2 inhibitors.
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Caturla F, Amat M, Reinoso RF, Calaf E, Warrellow G
Racemic and chiral sulfoxides as potential prodrugs of 4-pyrone COX-2 inhibitors.
Bioorg Med Chem Lett. 2006 Jul 1;16(13):3605-8. Epub 2006 May 2.
- PubMed ID
- 16647258 [ View in PubMed]
- 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.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Etoricoxib Prostaglandin G/H synthase 2 IC 50 (nM) 810 N/A N/A Details Rofecoxib Prostaglandin G/H synthase 2 IC 50 (nM) 760 N/A N/A Details