Synthesis and biological evaluation of 3-aminopyrrolidine derivatives as CC chemokine receptor 2 antagonists

Bioorg Med Chem Lett. 2010 Apr 1;20(7):2099-102. doi: 10.1016/j.bmcl.2010.02.072. Epub 2010 Feb 20.

Abstract

Novel 3-aminopyrrolidine derivatives were synthesized and evaluated for their antagonistic activity against human chemokine receptor 2. Structure-activity studies on 3-aminopyrrolidine incorporating heteroatomic carbocycle moieties led to piperidine compound 19, and piperazine compounds 42, 47 and 49 as highly potent hCCR2 antagonists.

MeSH terms

  • Cell Line
  • Chemotaxis / drug effects
  • Humans
  • Inhibitory Concentration 50
  • Protein Binding / drug effects
  • Pyrrolidines / chemical synthesis
  • Pyrrolidines / chemistry*
  • Pyrrolidines / pharmacology*
  • Receptors, CCR2 / antagonists & inhibitors*
  • Receptors, CCR2 / metabolism*
  • Structure-Activity Relationship

Substances

  • Pyrrolidines
  • Receptors, CCR2