Polyfluorinated bis-styrylbenzene beta-amyloid plaque binding ligands

J Med Chem. 2007 Oct 4;50(20):4986-92. doi: 10.1021/jm070085f. Epub 2007 Sep 11.

Abstract

beta-Amyloid (Abeta) binding affinities and specificities for six bis-styrylbenzenes with multiple magnetically equivalent fluorine atoms in the form of a tetrafluorophenyl core or symmetrical trifluoromethyl and trifluoromethoxy groups were determined by means of fluorescence titrations with amyloid peptide Abeta1-40 and a novel in vitro fluorescence-based assay using APP/PS1 transgenic mouse brain sections. Bis-styrylbenzenes with a tetrafluorophenyl core had increased Abeta binding affinities compared to their monofluorophenyl or phenyl counterparts. Bis-styrylbenzenes with carboxylic acid functional groups had lower Abeta binding affinities than their neutral counterparts. Selected bis-styrylbenzenes were demonstrated to have good blood-brain barrier penetration capabilities. These data extend the SAR of bis-styrylbenzene Abeta binding and provide direction for the development of a noninvasive probe for early detection of Alzheimer's disease using 19F MRI.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amyloid beta-Peptides / chemistry
  • Amyloid beta-Peptides / metabolism*
  • Animals
  • Blood-Brain Barrier / metabolism
  • Fluorescence
  • Fluorobenzenes / chemical synthesis
  • Fluorobenzenes / pharmacokinetics
  • Fluorobenzenes / pharmacology
  • Ligands
  • Mice
  • Mice, Transgenic
  • Peptide Fragments / chemistry
  • Peptide Fragments / metabolism*
  • Protein Binding
  • Stereoisomerism
  • Structure-Activity Relationship
  • Styrenes / chemical synthesis*
  • Styrenes / pharmacokinetics
  • Styrenes / pharmacology

Substances

  • Amyloid beta-Peptides
  • Fluorobenzenes
  • Ligands
  • Peptide Fragments
  • Styrenes
  • amyloid beta-protein (1-40)