The discovery of potent selective NPY Y(2) antagonists

Bioorg Med Chem Lett. 2013 Jul 15;23(14):4141-4. doi: 10.1016/j.bmcl.2013.05.038. Epub 2013 May 22.

Abstract

A series of small molecules with a piperidinyl core were synthesized and tested for binding affinity (IC50) at human Neuropeptide Y Y2 receptor. Various amide related analogs (ureas, reversed amides, and sulfonamides) were evaluated. Several potent and selective NPY Y2 antagonists were identified.

MeSH terms

  • Amides / chemical synthesis
  • Amides / chemistry*
  • Amides / metabolism
  • Animals
  • Drug Evaluation, Preclinical
  • Humans
  • Microsomes / metabolism
  • Protein Binding
  • Rats
  • Receptors, Neuropeptide Y / antagonists & inhibitors*
  • Receptors, Neuropeptide Y / metabolism
  • Sulfonamides / chemical synthesis
  • Sulfonamides / chemistry
  • Sulfonamides / metabolism
  • Urea / chemical synthesis
  • Urea / chemistry
  • Urea / metabolism

Substances

  • Amides
  • Receptors, Neuropeptide Y
  • Sulfonamides
  • neuropeptide Y2 receptor
  • Urea