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Bioorg Med Chem Lett
; 23(19): 5397-400, 2013 Oct 01.
Artículo
en Inglés
| MEDLINE
| ID: mdl-23981897
RESUMEN
In the last decade the inhibition of the enzyme 11ß-hydroxysteroid dehydrogenase 1 (11ß-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 11ß-HSD1 inhibitors bearing an arylsulfonylpiperazine scaffold. Optimization of the initial lead resulted in compound 11 that selectively inhibits 11ß-HSD1 (IC50=0.7 µM).