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ID: ALA2021804

Journal: Bioorg Med Chem Lett

Title: Synthesis and evaluation of piperidine urea derivatives as efficacious 11β-hydroxysteroid dehydrogenase type 1 inhibitors in diabetic ob/ob mice.

Authors: Zhang L, Chen J, Ning M, Zou Q, Leng Y, Shen J.

Abstract: 11β-Hydroxysteroid dehydrogenase type 1 (11β-HSD1) has attracted considerable attention as a potential target for the treatment of diabetes and metabolic syndrome. Herein we report the design, synthesis and efficacy evaluation of novel amide and urea 11β-HSD1 inhibitors. Structure-activity relationship studies led to the identification of 10c, which was efficacious in a diabetic ob/ob mouse model and reduced fasting and non-fasting blood glucose levels after ip dosing.

CiteXplore: 22440625

DOI: 10.1016/j.bmcl.2012.02.095