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

作　　者：DEUTHER-CONRAD Winnie BRUST Peter STEINBACH Jrg VERCOUILLIE Johnny 

机构地区：[1]Institute of Interdisciplinary Isotope Research

出　　处：《Science China Chemistry》2008年第5期457-463,共7页中国科学（化学英文版）

基　　金：the National Natural Science Foundation of China (Grant No. 20471011)

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 amine (16) show high binding affinities for the SERT with Ki values of 0.28 and 0.20 nmol·L-1,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.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-fluorophenoxy)-5-bromobenzenamine (15) and 2-(2-((dimethylamino)methyl)-4-fluorophenoxy)-5-iodobenzene amine (16) show high binding affinities for the SERT with K i values of 0.28 and 0.20 nmol·L?1, 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.

关 键 词：SEROTONIN TRANSPORTER DIPHENYL ETHER imaging agents in VITRO evaluation 

分 类 号：O641.4[理学—物理化学]