Various adamantane sulfonamides showed potent inhibitory activity against 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1). In continuation of our efforts to discover a more potent, selective and metabolically stable 11β-HSD1 inhibitor in mice as well as in humans, we optimized the adamantane sulfonamide using structure-based molecular modeling. Compound 3, which has alkyl side chains on the linker, demonstrated a potent inhibitory activity against human and mouse 11β-HSD1 (IC50 of 0.6 nM and 26 nM, respectively) and good physicochemical properties as a new anti-diabetes drug candidate.
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| http://dx.doi.org/10.1016/j.bmcl.2015.06.099 | DOI Listing |
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