| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1370522 | Bioorganic & Medicinal Chemistry Letters | 2015 | 6 Pages |
Abstract
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.
Graphical abstractBinding model of compound 3 with 11β-HSD1Figure optionsDownload full-size imageDownload as PowerPoint slide
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Sung Pyo Hong, Ky Youb Nam, Young June Shin, Kil Won Kim, Soon Kil Ahn,