Structure-activity relationships of non-imidazole H(3) receptor ligands. Part 1

Bioorg Med Chem Lett. 2002 Aug 5;12(15):2031-4. doi: 10.1016/s0960-894x(02)00309-8.

Abstract

SAR studies for novel non-imidazole containing H(3) receptor antagonists with high potency and selectivity for rat H(3) receptors are described. A high throughput screening lead, A-923, was further elaborated in a systematic manner to clarify a pharmacophore for this class of aryloxyalkyl piperazine based compounds.

MeSH terms

  • Amines / chemistry
  • Animals
  • Binding, Competitive
  • Carbamates / chemistry
  • Cerebral Cortex / metabolism
  • Histamine Antagonists / chemistry*
  • Histamine Antagonists / metabolism
  • Histamine Antagonists / pharmacology*
  • Humans
  • Ketones / chemistry*
  • Kinetics
  • Ligands
  • Piperazines / chemistry*
  • Rats
  • Receptors, Histamine H1 / metabolism
  • Receptors, Histamine H2 / metabolism
  • Receptors, Histamine H3 / drug effects*
  • Receptors, Histamine H3 / metabolism
  • Stereoisomerism
  • Structure-Activity Relationship

Substances

  • A-923 compound
  • Amines
  • Carbamates
  • Histamine Antagonists
  • Ketones
  • Ligands
  • Piperazines
  • Receptors, Histamine H1
  • Receptors, Histamine H2
  • Receptors, Histamine H3