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Abstract | Cited by

A series of α-sulfonamido-N-adamantanecarboxamide derivatives as 11β-HSD1 inhibitors was identified. Among them, compound 7j was the most active with an IC50 value of 8 nM in humans 11β-HSD1. Compound 7j exhibited reasonable stability, permeability and safety profiles (CYP and hERG). Compound 7j showed good ex vivo 11 β-HSD1 inhibition with ~80% inhibition after 20 MPK oral dosing.

Graphical abstract: Synthesis and biological evaluation of α-sulfonamido-N-adamantanecarboxamide derivatives as 11β-HSD1 inhibitors

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