2. Academic Validation
  3. Synthesis and evaluation of piperidine urea derivatives as efficacious 11β-hydroxysteroid dehydrogenase type 1 inhibitors in diabetic ob/ob mice

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

  • Bioorg Med Chem Lett. 2012 Apr 15;22(8):2748-52. doi: 10.1016/j.bmcl.2012.02.095.
Liming Zhang 1,  Junhua Chen,  Mengmeng Ning,  Qingan Zou,  Ying Leng,  Jianhua Shen
Affiliations

Affiliation

  • 1 State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, China.
PMID: 22440625 DOI: 10.1016/j.bmcl.2012.02.095
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.

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