2-(1H-Pyrazol-4-yl)acetic acids as CRTh2 antagonists

Bioorg Med Chem Lett. 2013 Jun 1;23(11):3349-53. doi: 10.1016/j.bmcl.2013.03.093. Epub 2013 Apr 2.

Abstract

High throughput screening identified the pyrazole-4-acetic acid substructure as CRTh2 receptor antagonists. Optimisation of the compounds uncovered a tight SAR but also identified some low nanomolar inhibitors.

MeSH terms

  • Acetates / chemical synthesis
  • Acetates / chemistry*
  • Acetates / pharmacokinetics
  • Animals
  • Half-Life
  • High-Throughput Screening Assays
  • Protein Binding
  • Pyrazoles / chemistry*
  • Rats
  • Receptors, Immunologic / antagonists & inhibitors*
  • Receptors, Immunologic / metabolism
  • Receptors, Prostaglandin / antagonists & inhibitors*
  • Receptors, Prostaglandin / metabolism
  • Structure-Activity Relationship

Substances

  • Acetates
  • Pyrazoles
  • Receptors, Immunologic
  • Receptors, Prostaglandin
  • pyrazole
  • prostaglandin D2 receptor