Azaindoles as potent CRTH2 receptor antagonists

Bioorg Med Chem Lett. 2011 Jan 15;21(2):841-5. doi: 10.1016/j.bmcl.2010.11.084. Epub 2010 Nov 21.

Abstract

A new class of 7-azaindole analogs of MK-7246 as potent and selective CRTH2 antagonists is reported. The SAR leading to the identification of the optimal azaindole regioisomer as well as the pharmacokinetics and off-target activities of the most potent antagonists are disclosed.

MeSH terms

  • Animals
  • Carbolines / chemistry
  • Humans
  • Indoles / chemistry*
  • Indoles / pharmacokinetics
  • Indoles / pharmacology*
  • Rats
  • Rats, Sprague-Dawley
  • Receptors, Immunologic / antagonists & inhibitors*
  • Receptors, Immunologic / metabolism*
  • Receptors, Prostaglandin / antagonists & inhibitors*
  • Receptors, Prostaglandin / metabolism*
  • Structure-Activity Relationship

Substances

  • ((7R)-7-(((4-fluorophenyl)sulfonyl)(methyl)amino)-6,7,8,9-tetrahydropyrido(1,2-a)indol-10-yl)acetic acid
  • 7-azaindole dimer
  • Carbolines
  • Indoles
  • Receptors, Immunologic
  • Receptors, Prostaglandin
  • prostaglandin D2 receptor