title: 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.affiliation: Department of Nuclear Medicine, Klinikum rechts der Isar, Technische Universität München, Ismaninger Strasse 22, D-81675 Munich, Germany. G.Henriksen@lrz.tum.de
authors.forename: Gjermund
authors.initials: G
authors.lastname: Henriksen
authors.forename: Andrea I
authors.initials: AI
authors.lastname: Hauser
authors.forename: Andrew D
authors.initials: AD
authors.lastname: Westwell
authors.forename: Behrooz H
authors.initials: BH
authors.lastname: Yousefi
authors.forename: Markus
authors.initials: M
authors.lastname: Schwaiger
authors.forename: Alexander
authors.initials: A
authors.lastname: Drzezga
authors.forename: Hans-Jürgen
authors.initials: HJ
authors.lastname: Wester
mesh_terms: D000818:Animals; D052160:Benzothiazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics; D001921:Brain / Q000378:metabolism; D002250:Carbon Radioisotopes; D051379:Mice; D008807:Mice, Inbred BALB C; D058225:Plaque, Amyloid / Q000378:metabolism*; D019275:Radiopharmaceuticals / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics; D013329:Structure-Activity Relationship; D014018:Tissue Distribution
chemical_list: D052160:Benzothiazoles; D002250:Carbon Radioisotopes; D019275:Radiopharmaceuticals