Synthesis and in vitro evaluation of new diphenyl ether derivatives as serotonin transporter ligands

• 来源期刊: 中国科学B辑（英文版）
• 年，卷（期）: 2008,（5）
• 页码范围: 457-463
• 页数: 7页
• 语种: 英文
• DOI: 10.1007/s11426-008-0007-6

摘要

For the development of new ligands as potential imaging agents for the serotonin transporter (SERT), a series of diphenyl ether derivatives have been synthesized, characterized, and evaluated for their in vitro binding affinities to the SERT. Among the above compounds, 2-(2-((dimethylamino)methyl)-4-fluoro-phenoxy)-5-bromobenzenamine (15) and 2-(2-((dimethylamino)methyl)-4-fluorophenoxy)-5-iodobenzene respectively. They can be further labeled with carbon-11, fluorine-18, iodine-123 or bromine-76, and evaluated as useful imaging agents for the SERT. Moreover, the study of the structure-activity relationship (SAR) provides some useful information for the future design of new ligands.