Design and synthesis of novel CCR3 antagonists

Bioorg Med Chem Lett. 2003 Oct 20;13(20):3597-600. doi: 10.1016/s0960-894x(03)00748-0.

Abstract

As part of our investigation into the development of potent CCR3 antagonists, a series of piperidine analogues was designed and prepared. Exploration of the piperidine core examined both the basicity and the location of a nitrogen, as well as conformational variants. The bicyclo-piperidine 24c was found to be the most potent inhibitor of CCR3 with an IC(50) of 0.0082 microM in the binding assay and 0.0024 microM in the chemotaxis assay.

MeSH terms

  • Drug Design
  • Piperidines / chemical synthesis
  • Piperidines / chemistry*
  • Receptors, CCR3
  • Receptors, Chemokine / antagonists & inhibitors*

Substances

  • Piperidines
  • Receptors, CCR3
  • Receptors, Chemokine