Push-pull benzothiazole derivatives as probes for detecting beta-amyloid plaques in Alzheimer's brains

Bioorg Med Chem. 2009 Oct 1;17(19):7002-7. doi: 10.1016/j.bmc.2009.08.032. Epub 2009 Aug 20.

Abstract

We synthesized push-pull benzothiazole derivatives and evaluated their potential as beta-amyloid imaging probes. In binding experiments in vitro, the benzothiazoles showed excellent affinity for synthetic Abeta(1-42) aggregates. beta-Amyloid plaques in the mouse and human brain were clearly visualized with the benzothiazoles, reflecting the results in vitro. These compounds may be a useful scaffold for the development of novel PET/SPECT and fluorescent tracers for detecting beta-amyloid in Alzheimer's brains.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Alzheimer Disease / diagnostic imaging*
  • Amyloid beta-Peptides / analysis*
  • Animals
  • Benzothiazoles / chemical synthesis*
  • Humans
  • Mice
  • Molecular Probe Techniques
  • Peptide Fragments / analysis*
  • Positron-Emission Tomography
  • Tomography, Emission-Computed, Single-Photon

Substances

  • Amyloid beta-Peptides
  • Benzothiazoles
  • Peptide Fragments
  • amyloid beta-protein (1-42)