2-Arylimidazo[2,1-b]benzothiazoles: a new family of amyloid binding agents with potential for PET and SPECT imaging of Alzheimer's brain

Bioorg Med Chem Lett. 2011 May 15;21(10):2966-8. doi: 10.1016/j.bmcl.2011.03.052. Epub 2011 Mar 21.

Abstract

We designed and synthesized a small series of 2-aryl-imidazo[2,1-b]benzothiazole, representing a combination of motifs from the two most potent amyloid imaging agents, PIB and IMPY. The binding affinity of the new compounds ranged from 6 to 133 nM. Among the best compounds, 3b (K(i)=6 nM) can be labeled with (11)CH(3) for PET imaging whereas 3j (K(i)=10.9 nM) can be labeled with (123)I for SPECT imaging.

MeSH terms

  • Alzheimer Disease / diagnosis*
  • Amyloid* / chemistry
  • Amyloid* / metabolism
  • Benzothiazoles / chemical synthesis*
  • Benzothiazoles / chemistry
  • Binding, Competitive
  • Biological Assay
  • Humans
  • Imidazoles / chemical synthesis*
  • Imidazoles / chemistry
  • Positron-Emission Tomography
  • Protein Binding
  • Tomography, Emission-Computed, Single-Photon

Substances

  • Amyloid
  • Benzothiazoles
  • Imidazoles
  • benzothiazole