Identification of a novel, orally bioavailable histamine H(3) receptor antagonist based on the 4-benzyl-(1H-imidazol-4-yl) template

Bioorg Med Chem Lett. 2002 Mar 25;12(6):937-41. doi: 10.1016/s0960-894x(02)00055-0.

Abstract

A novel series of histamine H(3) receptor antagonists, based on the 4-benzyl-(1H-imidazole-4-yl) template, incorporating urea and carbamate linkers has been prepared. Compound 3j is a selective H(3) antagonist and demonstrates excellent oral plasma levels in the rat and monkey.

MeSH terms

  • Administration, Oral
  • Animals
  • Biological Availability
  • Haplorhini
  • Histamine Antagonists / chemical synthesis*
  • Histamine Antagonists / pharmacokinetics
  • Histamine Antagonists / pharmacology
  • Imidazoles / chemical synthesis
  • Imidazoles / pharmacokinetics*
  • Imidazoles / pharmacology
  • Protein Binding
  • Rats
  • Receptors, Histamine H3 / drug effects
  • Receptors, Histamine H3 / metabolism*
  • Structure-Activity Relationship

Substances

  • Histamine Antagonists
  • Imidazoles
  • Receptors, Histamine H3