Abstract
A new series of cyclic sulfamide derivatives were synthesized and evaluated for their ability to inhibit 11β-HSD1. Among this series, 18e showed good in vitro activity toward human 11β-HSD1, selectivity against 11β-HSD2, microsomal stability, and pharmacokinetic and safety profiles (hERG, CYP, and acute toxicity). Additionally, 18e exhibited good in vivo efficacy in rat and monkey models.
Original language | English |
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Pages (from-to) | 88-93 |
Number of pages | 6 |
Journal | ACS Medicinal Chemistry Letters |
Volume | 3 |
Issue number | 2 |
DOIs | |
Publication status | Published - 2012 Feb 9 |
Keywords
- 11β-hydroxysteroid dehydrogenase type 1
- adamantyl group
- antidiabetic agents
- cyclic sulfamide
- diabetes
ASJC Scopus subject areas
- Biochemistry
- Drug Discovery
- Organic Chemistry