Discovery of (2S)-N-[(1R)-2-[4-cyclohexyl-4-[[(1,1-dimethylethyl)amino]carbonyl]-1-piperidinyl]-1-[(4-fluorophenyl)methyl]-2-oxoethyl]-4-methyl-2-piperazinecarboxamide (MB243), a potent and selective melanocortin subtype-4 receptor agonist

Bioorg Med Chem Lett. 2005 Jan 3;15(1):171-5. doi: 10.1016/j.bmcl.2004.10.020.

Abstract

We report the discovery and optimization of substituted 2-piperazinecarboxamides as potent and selective agonists of the melanocortin subtype-4 receptor. Further in vivo development of lead agonist, MB243, is disclosed.

MeSH terms

  • Animals
  • Dogs
  • Erectile Dysfunction / drug therapy
  • Haplorhini
  • Male
  • Mice
  • Obesity / drug therapy
  • Piperazines / chemistry
  • Piperazines / pharmacokinetics
  • Piperazines / pharmacology*
  • Piperazines / therapeutic use
  • Piperidines / chemistry
  • Piperidines / pharmacokinetics
  • Piperidines / pharmacology*
  • Piperidines / therapeutic use
  • Rats
  • Receptor, Melanocortin, Type 4 / agonists*

Substances

  • (2S)-N-((1R)-2-(4-cyclohexyl-4-(((1,1-dimethylethyl)amino)carbonyl)-1-piperidinyl)-1-((4-fluorophenyl)methyl)-2-oxoethyl)-4-methyl-2-piperazinecarboxamide
  • Piperazines
  • Piperidines
  • Receptor, Melanocortin, Type 4