Metabolically stabilized benzothiazoles for imaging of amyloid plaques.

Abstract

Six new N-11C-labeled aminophenylbenzothiazoles substituted with fluorine in different positions have been synthesized and evaluated as amyloid-beta binding ligands. Our structure-property relationship studies show that the substitution pattern of the phenyl ring and the benzothiazole moiety has an influence on the metabolic stability, which in turn has an effect on the brain uptake kinetics. Two lead compounds have been identified with improved physicochemical characteristics for Abeta-plaque imaging in vivo.

• Authors: Gjermund Henriksen, Andrea I Hauser, Andrew D Westwell, Behrooz H Yousefi, Markus Schwaiger, Alexander Drzezga, Hans-Jürgen Wester
• Journal: Journal of medicinal chemistry (J Med Chem) Vol. 50 Issue 6 Pg. 1087-9 (Mar 22 2007) ISSN: 0022-2623 [Print] United States
• PMID: 17319654 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Benzothiazoles
• Carbon Radioisotopes
• Radiopharmaceuticals

Topics

• Animals
• Benzothiazoles (chemical synthesis, chemistry, pharmacokinetics)
• Brain (metabolism)
• Carbon Radioisotopes
• Mice
• Mice, Inbred BALB C
• Plaque, Amyloid (metabolism)
• Radiopharmaceuticals (chemical synthesis, chemistry, pharmacokinetics)
• Structure-Activity Relationship
• Tissue Distribution