Metabolically stabilized benzothiazoles for imaging of amyloid plaques

被引：85

作者：

Henriksen, Gjermund

Hauser, Andrea I.

Westwell, Andrew D.

Yousefi, Behrooz H.

Schwaiger, Markus

Drzezga, Alexander

Wester, Hans-Juergen

机构：

[1] Tech Univ Munich, Klinikum Rechts Isar, Dept Nucl Med, D-81675 Munich, Germany

[2] Cardiff Univ, Welsh Sch Pharm, Cardiff CF10 3XF, S Glam, Wales

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2007年 / 50卷 / 06期

关键词：

D O I：

10.1021/jm061466g

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Six new N-C-11-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 A beta-plaque imaging in vivo.

引用

页码：1087 / 1089

页数：3

共 14 条

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