695221-93-3Relevant academic research and scientific papers
Synthesis and biological analysis of benzazol-2-yl piperazine sulfonamides as 11β-hydroxysteroid dehydrogenase 1 inhibitors
Hofer, Sandra,Kratschmar, Denise V.,Schernthanner, Brigitte,Vuorinen, Anna,Schuster, Daniela,Odermatt, Alex,Easmon, Johnny
, p. 5397 - 5400 (2013)
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).
