Parallel solution- and solid-phase synthesis of spiropyrrolo-pyrroles as novel neurokinin receptor ligands

Bioorg Med Chem Lett. 2002 Nov 4;12(21):3073-6. doi: 10.1016/s0960-894x(02)00659-5.

Abstract

The combination of a 3,5-bis(trifluoromethyl)phenyl needle with the spiropyrrolo-pyrrole motive as a privileged GPCR scaffold was the basis for designing a focused combinatorial library targeted towards the neurokinin-1 receptor. A solution- and solid-phase method is described and binding affinities of representative compounds are presented.

MeSH terms

  • Combinatorial Chemistry Techniques
  • GTP-Binding Proteins / metabolism
  • Indicators and Reagents
  • Ligands
  • Pyrroles / chemical synthesis*
  • Pyrroles / pharmacology*
  • Receptors, Neurokinin-1 / drug effects
  • Receptors, Neurokinin-1 / metabolism*
  • Receptors, Neurokinin-2 / drug effects
  • Receptors, Neurokinin-2 / metabolism*
  • Receptors, Neurokinin-3 / drug effects
  • Receptors, Neurokinin-3 / metabolism*
  • Structure-Activity Relationship

Substances

  • Indicators and Reagents
  • Ligands
  • Pyrroles
  • Receptors, Neurokinin-1
  • Receptors, Neurokinin-2
  • Receptors, Neurokinin-3
  • GTP-Binding Proteins