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Synthesis and biological evaluation of cyclic sulfamide derivatives as 11β-hydroxysteroid dehydrogenase 1 inhibitors.
- Source :
-
ACS medicinal chemistry letters [ACS Med Chem Lett] 2012 Jan 17; Vol. 3 (2), pp. 88-93. Date of Electronic Publication: 2012 Jan 17 (Print Publication: 2012). - Publication Year :
- 2012
-
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.
Details
- Language :
- English
- ISSN :
- 1948-5875
- Volume :
- 3
- Issue :
- 2
- Database :
- MEDLINE
- Journal :
- ACS medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 24900439
- Full Text :
- https://doi.org/10.1021/ml200226x