Ureas with histamine H3-antagonist receptor activity--a new scaffold discovered by lead-hopping from cinnamic acid amides

Bioorg Med Chem Lett. 2006 Oct 15;16(20):5303-8. doi: 10.1016/j.bmcl.2006.07.093.

Abstract

A group of tri and tetrasubstituted urea derivatives have been found to be hH(3)-antagonists. The most potent compounds were found in the class of (piperazine-1-yl)-(piperidine-1-yl)-methanones which in addition showed negligible hERG inhibition.

MeSH terms

  • Cinnamates / chemistry*
  • ERG1 Potassium Channel
  • Ether-A-Go-Go Potassium Channels / antagonists & inhibitors
  • Histamine Antagonists / chemical synthesis
  • Histamine Antagonists / chemistry
  • Histamine Antagonists / pharmacology*
  • Humans
  • Molecular Structure
  • Receptors, Histamine H3 / drug effects*
  • Stereoisomerism
  • Structure-Activity Relationship
  • Thiazines / chemical synthesis
  • Thiazines / chemistry
  • Thiazines / pharmacology*
  • Urea / analogs & derivatives*
  • Urea / chemical synthesis
  • Urea / chemistry*
  • Urea / pharmacology

Substances

  • Cinnamates
  • ERG1 Potassium Channel
  • Ether-A-Go-Go Potassium Channels
  • Histamine Antagonists
  • KCNH2 protein, human
  • Receptors, Histamine H3
  • Thiazines
  • Urea