New amide derivatives as melanin-concentrating hormone receptor 1 antagonists for the treatment of obesity

Arzneimittelforschung. 2008;58(11):585-91. doi: 10.1055/s-0031-1296561.

Abstract

Melanin-concentrating hormone (MCH) is a recently discovered central nervous system (CNS) target for treating obesity. Two novel series of amide derivatives were synthesized and evaluated biologically as MCH-R1 (melanin-concentrating hormone receptor 1) antagonists. The results showed that diphenyl substituents on the amide lead to better activity than biphenyl substituents.

MeSH terms

  • Amides / chemical synthesis*
  • Amides / pharmacology*
  • Animals
  • Anti-Obesity Agents / chemical synthesis*
  • Anti-Obesity Agents / pharmacology*
  • CHO Cells
  • Cricetinae
  • Cricetulus
  • Humans
  • Indicators and Reagents
  • Receptors, Somatostatin / antagonists & inhibitors*
  • Solvents
  • Structure-Activity Relationship

Substances

  • Amides
  • Anti-Obesity Agents
  • Indicators and Reagents
  • MCHR1 protein, human
  • Receptors, Somatostatin
  • Solvents