Design, synthesis and structure-activity relationship of rhenium 2-arylbenzothiazoles as β-amyloid plaque binding agents.

@article{Pan2013DesignSA,
  title={Design, synthesis and structure-activity relationship of rhenium 2-arylbenzothiazoles as β-amyloid plaque binding agents.},
  author={Jinhe Pan and N. Scott Mason and Manik L. Debnath and Chester A. Mathis and William E. Klunk and Kuo-Shyan Lin},
  journal={Bioorganic & medicinal chemistry letters},
  year={2013},
  volume={23 6},
  pages={1720-6}
}
To continue our efforts toward the development of (99m)Tc PiB analogs, we have synthesized 24 neutral and lipophilic Re (as a surrogate of (99m)Tc) 2-arylbenzothiazoles, and explored their structure-activity relationship for binding to Aβ1-40 fibrils. These Re complexes were designed and synthesized via the integrated approach, so their (99m)Tc analogs would have a greater chance of crossing the blood-brain barrier. While the lipophilicities (logPC18=1.59-3.53) of these Re 2-arylbenzothiazoles… CONTINUE READING