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.
Bibliographical noteFunding 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 .
- 11β-Hydroxysteroid dehydrogenase 1
- Cyclic sulfonamide
ASJC Scopus subject areas
- Molecular Medicine
- Molecular Biology
- Pharmaceutical Science
- Drug Discovery
- Clinical Biochemistry
- Organic Chemistry