Synthesis of carbon-11 and fluorine-18 labeled N-acetyl-l-aryl-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinolinederivatives as new potential PET AMPA receptor ligands

被引:50
作者
Gao, M
Kong, DY
Clearfield, A
Zheng, QH [1 ]
机构
[1] Indiana Univ, Sch Med, Dept Radiol, Indianapolis, IN 46202 USA
[2] Texas A&M Univ, Dept Chem, College Stn, TX 77843 USA
关键词
N-acetyl-1-aryl-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline; derivatives; carbon-11; fluorine-18; positron emission tomography; 2-amino-3-(3-hydroxy-5-methylisoxazol-4-yl)propionic acid; receptor; brain diseases;
D O I
10.1016/j.bmcl.2006.01.042
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
New carbon-11 and fluorine-18 labeled N-acetyl-1-aryl-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline derivatives were designed and synthesized as potential positron emission tomography AMPA (2-amino-3-(3-hydroxy-5-methylisoxazol-4-yl)propionic acid) receptor ligands to image brain diseases. The single crystal structure of the most potent compound N-acetyl-1-(4'-chlorophenyl)-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline (5a) is first reported. (C) 2006 Elsevier Ltd. All rights reserved.
引用
收藏
页码:2229 / 2233
页数:5
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