Racemic and chiral sulfoxides as potential prodrugs of the COX-2 inhibitors Vioxx® and Arcoxia®

…, M Amat, RF Reinoso, M Córdoba, G Warrellow

文献索引：Caturla, Francisco; Amat, Merce; Reinoso, Raquel F.; Cordoba, Monica; Warrellow, Graham Bioorganic and Medicinal Chemistry Letters, 2006 , vol. 16, # 12 p. 3209 - 3212

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被引用次数: 25

摘要

The preparation of the sulfoxide analogues 2 and 4, and their enantiomeric pure forms is discussed as well as their potential to act as prodrugs to the potent and selective sulfone- containing COX-2 inhibitors rofecoxib and etoricoxib. Sulfoxides 2 and 4 were shown to be effectively transformed in vivo into rofecoxib and etoricoxib, respectively, after oral administration in rats. In the case of sulfoxide 2, both a slightly improved pharmacokinetic ...