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

…, DV Kratschmar, B Schernthanner, A Vuorinen…

文献索引：Hofer, Sandra; Kratschmar, Denise V.; Schernthanner, Brigitte; Vuorinen, Anna; Schuster, Daniela; Odermatt, Alex; Easmon, Johnny Bioorganic and Medicinal Chemistry Letters, 2013 , vol. 23, # 19 p. 5397 - 5400

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被引用次数: 7

摘要

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 ...