Discovery of novel, orally available benzimidazoles as melanin concentrating hormone receptor 1 (MCHR1) antagonists

Bioorg Med Chem Lett. 2010 Sep 15;20(18):5443-8. doi: 10.1016/j.bmcl.2010.07.086. Epub 2010 Jul 29.

Abstract

Melanin concentrating hormone (MCH) is an important mediator of energy homeostasis and plays role in several disorders such as obesity, stress, depression and anxiety. The synthesis and biological evaluation of novel benzimidazole derivatives as MCHR1 antagonists are described. The in vivo proof of principle for weight loss with a lead compound from this series is exemplified.

MeSH terms

  • Animals
  • Anti-Obesity Agents / chemical synthesis
  • Anti-Obesity Agents / chemistry*
  • Anti-Obesity Agents / pharmacology
  • Anti-Obesity Agents / therapeutic use*
  • Benzimidazoles / chemical synthesis
  • Benzimidazoles / chemistry*
  • Benzimidazoles / pharmacology
  • Benzimidazoles / therapeutic use*
  • Humans
  • Mice
  • Mice, Inbred C57BL
  • Models, Molecular
  • Obesity / drug therapy*
  • Protein Binding
  • Receptors, Somatostatin / antagonists & inhibitors*
  • Receptors, Somatostatin / metabolism*
  • Weight Loss / drug effects

Substances

  • Anti-Obesity Agents
  • Benzimidazoles
  • MCHR1 protein, human
  • Receptors, Somatostatin