Identification of a sulfonamide series of CCR2 antagonists

Bioorg Med Chem Lett. 2010 Jul 1;20(13):3961-4. doi: 10.1016/j.bmcl.2010.04.142. Epub 2010 May 7.

Abstract

A series of sulfonamide CCR2 antagonists was identified by high-throughput screening. Management of molecular weight and physical properties, in particular moderation of lipophilicity and study of pK(a), yielded highly potent CCR2 antagonists exhibiting good pharmacokinetic properties and improved potency in the presence of human plasma.

MeSH terms

  • Animals
  • Dose-Response Relationship, Drug
  • High-Throughput Screening Assays
  • Humans
  • Mice
  • Molecular Structure
  • Receptors, CCR1 / antagonists & inhibitors
  • Receptors, CCR2 / antagonists & inhibitors*
  • Stereoisomerism
  • Structure-Activity Relationship
  • Sulfonamides / chemistry
  • Sulfonamides / pharmacology*

Substances

  • Receptors, CCR1
  • Receptors, CCR2
  • Sulfonamides