Abstract
A new series of cyclic sulfonamide derivatives was synthesized and evaluated for their ability to inhibit 11β-HSD1. Cyclic sulfonamides with phenylacetyl substituents at the 2-position showed nanomolar inhibitory activities. Among them, compound 4e exhibited a good in vitro inhibitory activity and selectivity toward human 11β-HSD2.
Original language | English |
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Pages (from-to) | 1065-1069 |
Number of pages | 5 |
Journal | Bioorganic and Medicinal Chemistry Letters |
Volume | 20 |
Issue number | 3 |
DOIs | |
Publication status | Published - 2010 Feb 1 |
Bibliographical note
Funding Information:This research was supported by the Center for Biological Modulators of the 21st Century Frontier R&D Program , Ministry of Education, Science and Technology, Korea .
Keywords
- 11β-Hydroxysteroid dehydrogenase 1
- Cyclic sulfonamide
- Diabetes
- Inhibitor
ASJC Scopus subject areas
- Biochemistry
- Molecular Medicine
- Molecular Biology
- Pharmaceutical Science
- Drug Discovery
- Clinical Biochemistry
- Organic Chemistry