Design, synthesis, and structure-activity relationship of novel thiophene derivatives for beta-amyloid plaque imaging

Bioorg Med Chem Lett. 2006 Mar 1;16(5):1350-2. doi: 10.1016/j.bmcl.2005.11.055. Epub 2005 Dec 1.


Novel 2,5-diphenylthiophene derivatives were synthesized and structure activity relationship with regard to Abeta plaque binding was studied. Binding affinities of these compounds were found to range from 3.9 to >1000 nM, depending on the substitution patterns on the phenyl ring. The fluoroethyl-substituted thiophene derivatives showed excellent binding affinities. These compounds may be useful for the development of novel PET tracers for the imaging of beta-amyloid plaques in the brain of patients with Alzheimer's disease.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Alzheimer Disease / diagnosis
  • Alzheimer Disease / metabolism*
  • Amyloid beta-Peptides / analysis
  • Amyloid beta-Peptides / metabolism*
  • Animals
  • Cell Line
  • Drug Design*
  • Ligands
  • Mice
  • Molecular Structure
  • Structure-Activity Relationship
  • Thiophenes / chemical synthesis
  • Thiophenes / chemistry*
  • Thiophenes / pharmacology*


  • Amyloid beta-Peptides
  • Ligands
  • Thiophenes