Discovery of a new class of non-imidazole oxazoline-based histamine H(3) receptor (H(3)R) inverse agonists

ChemMedChem. 2009 Jul;4(7):1063-8. doi: 10.1002/cmdc.200900055.

Abstract

H(3)R inverse agonists based on an aminopropoxy-phenyloxazoline framework constitute highly valuable druglike lead compounds that display efficacy in a mouse model of recognition memory.

MeSH terms

  • Animals
  • CHO Cells
  • Caco-2 Cells
  • Cell Line
  • Cricetinae
  • Cricetulus
  • Drug Design
  • Drug Inverse Agonism
  • Histamine H3 Antagonists / chemical synthesis
  • Histamine H3 Antagonists / chemistry
  • Histamine H3 Antagonists / pharmacology*
  • Humans
  • Imidazoles / chemistry
  • Mice
  • Oxazoles / chemical synthesis
  • Oxazoles / chemistry
  • Oxazoles / pharmacology*
  • Prefrontal Cortex / drug effects
  • Rats
  • Rats, Wistar
  • Receptors, Histamine H3 / chemistry*
  • Receptors, Histamine H3 / metabolism
  • Structure-Activity Relationship

Substances

  • Histamine H3 Antagonists
  • Imidazoles
  • Oxazoles
  • Receptors, Histamine H3
  • imidazole