Hofer, Sandra and Kratschmar, Denise V. and Schernthanner, Brigitte and Vuorinen, Anna and Schuster, Daniela and Odermatt, Alex and Easmon, Johnny. (2013) Synthesis and biological analysis of benzazol-2-yl piperazine sulfonamides as 11β-hydroxysteroid dehydrogenase 1 inhibitors. Bioorganic and Medicinal Chemistry Letters, 23 (19). pp. 5397-5400.
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Official URL: http://edoc.unibas.ch/49603/
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Abstract
In the last decade the inhibition of the enzyme 11β-hydroxysteroid dehydrogenase 1 (11β-HSD1) emerged as a promising new strategy to treat diabetes and several metabolic syndrome phenotypes. Using a molecular modeling approach and classical bioisosteric studies, we discovered a new class of 11β-HSD1 inhibitors bearing an arylsulfonylpiperazine scaffold. Optimization of the initial lead resulted in compound 11 that selectively inhibits 11β-HSD1 (IC50=0.7 μM).
| Faculties and Departments: | 05 Faculty of Science > Departement Pharmazeutische Wissenschaften > Pharmazie > Molecular and Systems Toxicology (Odermatt) |
|---|---|
| UniBasel Contributors: | Odermatt, Alex and Kratschmar, Denise |
| Item Type: | Article, refereed |
| Article Subtype: | Research Article |
| Publisher: | Elsevier |
| ISSN: | 0960-894X |
| e-ISSN: | 1464-3405 |
| Note: | Publication type according to Uni Basel Research Database: Journal article |
| Identification Number: |
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| Last Modified: | 01 Dec 2017 08:47 |
| Deposited On: | 01 Dec 2017 08:47 |
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