Azabicyclic sulfonamides as potent 11beta-HSD1 inhibitors
| Autor: | Shah Unmesh G, Giuseppe Terracina, Julie Lee, Craig D. Boyle, Lili Zhang, Hana E. Baker, Timothy J. Kowalski, Samuel Chackalamannil |
|---|---|
| Rok vydání: | 2009 |
| Předmět: |
Clinical Biochemistry
Pharmaceutical Science 11β hsd1 Biochemistry 11β hsd1 inhibitors Mice Structure-Activity Relationship In vivo Drug Discovery 11-beta-Hydroxysteroid Dehydrogenase Type 1 medicine Animals Humans Hypoglycemic Agents Enzyme Inhibitors Molecular Biology Sulfonamides Chemistry Organic Chemistry Sulfonamide (medicine) Cortisone Molecular Medicine Azabicyclo Compounds hormones hormone substitutes and hormone antagonists medicine.drug |
| Zdroj: | Bioorganicmedicinal chemistry letters. 20(5) |
| ISSN: | 1464-3405 |
| Popis: | Inhibition of 11β-HSD1 has demonstrated potential in the treatment of various components of metabolic syndrome. We wish to report herein the discovery of novel azabicyclic sulfonamide based 11β-HSD1 inhibitors. Highly potent compounds exhibiting inhibitory activities at both human and mouse 11β-HSD1 were identified. Several compounds demonstrated significant in vivo activity in the mouse cortisone challenge assay. |
| Databáze: | OpenAIRE |
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