Racemic and chiral sulfoxides as potential prodrugs of 4-pyrone COX-2 inhibitors |
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Authors: | Caturla Francisco Amat Mercè Reinoso Raquel F Calaf Elena Warrellow Graham |
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Affiliation: | Department of Medicinal Chemistry, Almirall Prodesfarma S.A., Research Center, Cardener 68-74, 08024 Barcelona, Spain. jfcaturl@almirall.es |
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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. |
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