Non-imidazole heterocyclic histamine H3 receptor antagonists

Bioorg Med Chem Lett. 2003 May 19;13(10):1767-70. doi: 10.1016/s0960-894x(03)00299-3.

Abstract

Continued exploration of the SAR around the lead imidazopyridine histamine H(3) antagonist 1 has led to the discovery of several related series of heterocyclic histamine H(3) antagonists. The synthesis and SAR of indolizine, indole and pyrazolopyridine based compounds are now described.

MeSH terms

  • Animals
  • Biotransformation
  • Cell Line
  • Cell Membrane Permeability
  • Drug Stability
  • Heterocyclic Compounds, 4 or More Rings / chemical synthesis*
  • Heterocyclic Compounds, 4 or More Rings / pharmacokinetics
  • Heterocyclic Compounds, 4 or More Rings / pharmacology
  • Histamine Antagonists / chemical synthesis*
  • Histamine Antagonists / pharmacokinetics*
  • Histamine Antagonists / pharmacology
  • Humans
  • Indoles / chemical synthesis
  • Indoles / pharmacology
  • Indolizines / chemical synthesis
  • Indolizines / pharmacology
  • Microsomes, Liver
  • Pyrazoles / chemical synthesis
  • Pyrazoles / pharmacology
  • Pyridines / chemical synthesis
  • Pyridines / pharmacology
  • Rats
  • Receptors, Histamine H3*
  • Structure-Activity Relationship

Substances

  • Heterocyclic Compounds, 4 or More Rings
  • Histamine Antagonists
  • Indoles
  • Indolizines
  • Pyrazoles
  • Pyridines
  • Receptors, Histamine H3
  • pyrazolopyridine