Pyrazolone methylamino piperidine derivatives as novel CCR3 antagonists

Bioorg Med Chem Lett. 2007 Aug 1;17(15):4228-31. doi: 10.1016/j.bmcl.2007.05.035. Epub 2007 May 17.

Abstract

The discovery and optimization of a novel class of potent CCR3 antagonists is described. Details of synthesis and SAR are given together with some ADME properties of selected compounds. An optimal balance between activities, physicochemical properties, and in vitro metabolic stability was reached by the proper choice of substituents.

MeSH terms

  • Humans
  • Piperidines / chemical synthesis
  • Piperidines / chemistry
  • Piperidines / pharmacology*
  • Receptors, CCR3
  • Receptors, Chemokine / antagonists & inhibitors*
  • Structure-Activity Relationship

Substances

  • CCR3 protein, human
  • Piperidines
  • Receptors, CCR3
  • Receptors, Chemokine