Metabolically stabilized benzothiazoles for imaging of amyloid plaques

Gjermund Henriksen; Andrea I. Hauser; Andrew D. Westwell; Behrooz H. Yousefi; Markus Schwaiger; Alexander Drzezga; Hans Jürgen Wester

doi:10.1021/jm061466g

Metabolically stabilized benzothiazoles for imaging of amyloid plaques

Gjermund Henriksen, Andrea I. Hauser, Andrew D. Westwell, Behrooz H. Yousefi, Markus Schwaiger, Alexander Drzezga, Hans Jürgen Wester

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92 Scopus citations

Abstract

Six new N-¹¹C-labeled aminophenylbenzothiazoles substituted with fluorine in different positions have been synthesized and evaluated as amyloid-β 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 Aβ-plaque imaging in vivo.

Original language	English
Pages (from-to)	1087-1089
Number of pages	3
Journal	Journal of Medicinal Chemistry
Volume	50
Issue number	6
DOIs	https://doi.org/10.1021/jm061466g
State	Published - 22 Mar 2007

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author = "Gjermund Henriksen and Hauser, {Andrea I.} and Westwell, {Andrew D.} and Yousefi, {Behrooz H.} and Markus Schwaiger and Alexander Drzezga and Wester, {Hans J{\"u}rgen}",

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AU - Henriksen, Gjermund

AU - Hauser, Andrea I.

AU - Westwell, Andrew D.

AU - Yousefi, Behrooz H.

AU - Schwaiger, Markus

AU - Drzezga, Alexander

AU - Wester, Hans Jürgen

PY - 2007/3/22

Y1 - 2007/3/22

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AB - Six new N-11C-labeled aminophenylbenzothiazoles substituted with fluorine in different positions have been synthesized and evaluated as amyloid-β 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 Aβ-plaque imaging in vivo.

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Metabolically stabilized benzothiazoles for imaging of amyloid plaques

Abstract

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