Tetrahydroquinoline derivatives as CRTH2 antagonists

Bioorg Med Chem Lett. 2009 Dec 15;19(24):6840-4. doi: 10.1016/j.bmcl.2009.10.094. Epub 2009 Oct 25.

Abstract

A series of tetrahydroquinoline-derived inhibitors of the CRTH2 receptor was discovered by a high throughput screen. Optimization of these compounds for potency and pharmacokinetic properties led to the discovery of potent and orally bioavailable CRTH2 antagonists.

MeSH terms

  • Anti-Allergic Agents / chemistry*
  • Anti-Allergic Agents / pharmacokinetics
  • Anti-Allergic Agents / pharmacology
  • Cell Line
  • Cell Shape / drug effects
  • Drug Discovery
  • Eosinophils / drug effects
  • Eosinophils / immunology
  • Humans
  • Quinolines / chemistry*
  • Quinolines / pharmacokinetics
  • Quinolines / pharmacology
  • Receptors, Immunologic / antagonists & inhibitors*
  • Receptors, Prostaglandin / antagonists & inhibitors*

Substances

  • Anti-Allergic Agents
  • Quinolines
  • Receptors, Immunologic
  • Receptors, Prostaglandin
  • 1,2,3,4-tetrahydroquinoline
  • prostaglandin D2 receptor