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Synthesis and biological analysis of benzazol-2-yl piperazine sulfonamides as 11β-hydroxysteroid dehydrogenase 1 inhibitors

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:
Last Modified:01 Dec 2017 08:47
Deposited On:01 Dec 2017 08:47

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