Design, synthesis, and SAR studies on a series of 2-pyridinylpiperazines as potent antagonists of the melanocortin-4 receptor

Bioorg Med Chem Lett. 2006 Jul 15;16(14):3693-6. doi: 10.1016/j.bmcl.2006.04.069. Epub 2006 May 11.

Abstract

A series of 2-pyridinylpiperazines derived from beta-Ala-(2,4-Cl)Phe dipeptide was synthesized for the study of their SARs and possible interactions with the MC4 receptor. Compounds such as 11k (Ki=6.5 nM) possessed high potency.

MeSH terms

  • Dipeptides / chemistry
  • Drug Design
  • Humans
  • Piperazines / chemical synthesis*
  • Piperazines / pharmacology*
  • Pyridines / chemical synthesis*
  • Pyridines / pharmacology*
  • Receptor, Melanocortin, Type 4 / antagonists & inhibitors*
  • Structure-Activity Relationship
  • beta-Alanine / chemistry

Substances

  • Dipeptides
  • Piperazines
  • Pyridines
  • Receptor, Melanocortin, Type 4
  • beta-Alanine