Discovery of substituted phenyl urea derivatives as novel long-acting β2-adrenoreceptor agonists

Bioorg Med Chem Lett. 2011 Mar 1;21(5):1545-8. doi: 10.1016/j.bmcl.2010.12.096. Epub 2011 Jan 6.

Abstract

The synthesis of diverse functionalized ureas in a semi-parallel fashion is described, as well as their β(1)/β(2)-adrenergic activities and the corresponding structure-activity relationship (SAR). We have focused on lipophilicity and duration of action, and we have discovered a strong correlation in this series of molecules. A quantitative structure-activity relationship (QSAR) analysis will be presented that quantifies this relationship.

MeSH terms

  • Adrenergic beta-2 Receptor Agonists
  • Drug Discovery*
  • Molecular Structure
  • Phenol / chemical synthesis*
  • Phenol / chemistry
  • Phenol / pharmacology
  • Quantitative Structure-Activity Relationship
  • Urea / chemical synthesis*
  • Urea / chemistry
  • Urea / pharmacology

Substances

  • Adrenergic beta-2 Receptor Agonists
  • Phenol
  • Urea