Pre-clinical characterization of aryloxypyridine amides as histamine H3 receptor antagonists: identification of candidates for clinical development

Bioorg Med Chem Lett. 2010 Jul 15;20(14):4210-4. doi: 10.1016/j.bmcl.2010.05.041. Epub 2010 May 16.

Abstract

The pre-clinical characterization of novel aryloxypyridine amides that are histamine H(3) receptor antagonists is described. These compounds are high affinity histamine H(3) ligands that penetrate the CNS and occupy the histamine H(3) receptor in rat brain. Several compounds were extensively profiled pre-clinically leading to the identification of two compounds suitable for nomination as development candidates.

MeSH terms

  • Amides / chemistry
  • Animals
  • Azepines / chemistry
  • Azepines / pharmacology*
  • Drug Evaluation, Preclinical
  • Histamine H3 Antagonists / pharmacology*
  • Pyridines / chemistry
  • Pyridines / pharmacology*
  • Rats

Substances

  • (4-cyclobutyl-(1,4)diazepan-1-yl)-(6-(4-fluorophenoxy)pyridin-3-yl)methanone
  • Amides
  • Azepines
  • Histamine H3 Antagonists
  • Pyridines