Synthesis and 11-beta hydroxysteroid dehydrogenase 1 inhibition of thiazolidine derivatives with an adamantyl group

Literature Life Science

In vitro inhibitory activity of 11β-HSD1assessed with the use of a HTRF cortisol assay


A new series of thiazolidine derivatives with an adamantyl group was synthesized and evaluated for their ability to inhibit 11ß-hydroxysteroid dehydrogenase 1 (11ß-HSD1). Our initial compound 5a showed a weak inhibitory activity. Significant improvements in potency were achieved by substituent modification. The potent compound 8g (E) showed good in vitro inhibitory activity toward human 11ß-HSD1, selectivity toward 11ß-HSD2, metabolic stability, pharmacokinetic, and safety profile. Furthermore, this compound significantly inhibited 11ß-HSD1 activity in rat and monkey models, and showed improved glycemic control in KKAy mice.


Bioorg Med Chem Lett. 2011;21(1):435-9.

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