Synthesis of Potent and Orally Efficacious 11β-Hydroxysteroid Dehydrogenase Type 1 Inhibitor HSD-016

Cortisol and the glucocorticoid receptor (GR) signaling pathway has been linked to the development of diabetes and metabolic syndrome. In vivo, 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) catalyzes the conversion of inactive cortisone to its active form, cortisol. Existing clinical data have...

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Veröffentlicht in:	Journal of organic chemistry 2011-09, Vol.76 (17), p.7048-7055
Hauptverfasser:	Wan, Zhao-Kui, Chenail, Eva, Li, Huan-Qiu, Kendall, Christopher, Wang, Youchu, Gingras, Stéphane, Xiang, Jason, Massefski, Walter W, Mansour, Tarek, S, Saiah, Eddine
Format:	Artikel
Sprache:	eng
Schlagworte:	11-beta-Hydroxysteroid Dehydrogenase Type 1 - antagonists & inhibitors 11-beta-Hydroxysteroid Dehydrogenase Type 1 - chemical synthesis 11-beta-Hydroxysteroid Dehydrogenase Type 1 - chemistry Administration, Oral Alicyclic compounds, terpenoids, prostaglandins, steroids Chemistry Enzyme Activation - drug effects Enzyme Inhibitors - chemical synthesis Enzyme Inhibitors - chemistry Enzyme Inhibitors - pharmacology Exact sciences and technology Heterocyclic compounds Heterocyclic compounds with several n hetero atoms in the same ring, in separated rings or in fused rings Humans Molecular Structure Organic chemistry Piperazines - chemical synthesis Piperazines - chemistry Piperazines - pharmacology Preparations and properties Propanols - chemical synthesis Propanols - chemistry Propanols - pharmacology Steroids
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