Novel glucocorticoid antedrugs possessing a 21-(γ-lactone) ring

RM Angell, K Biggadike, RM Farrell, SS Flack…

Index: Angell, Richard M.; Biggadike, Keith; Farrell, Rosanne M.; Flack, Stephen S.; Hancock, Ashley P.; Irving, Wendy R.; Lynn, Sean M.; Procopiou, Panayiotis A. Journal of the Chemical Society. Perkin Transactions 1, 2002 , # 6 p. 831 - 839

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Citation Number: 9

Abstract

A series of novel pregnane derivatives bearing γ-butyrolactones at C21 were prepared and tested as glucocorticoid agonists. The compounds were also tested for their lability in human plasma, and found to be rapidly hydrolysed by the enzyme paraoxonase to the respective hydroxyacids.