bis-Pyridinium cyclophanes: novel ligands with high affinity for the blood-brain barrier choline transporter.
摘要：
A series of pyridinium cyclophane analogs designed as conformationally restricted -quaternary ammonium compounds were evaluated for their affinity for the blood–brain barrier (BBB) choline transporter. All the cyclophanes investigated exhibited high affinity compared to choline. Of these compounds, , ′-(1,10-decanediyl)3,3′-(1,9-decadiyn-1,10-diyl)-pyridinium diiodide () and ,′-(1,9-nonanediyl)3,3′-(1,9-decadiyn-1,10-diyl)-pyridinium dibromide () exhibited highest affinity with values of 0.8μM and 1.4μM, respectively, and constitute some of the most potent BBB choline transporter ligands reported.Graphical abstractbis) designed as conformationally restricted -quaternary ammonium compounds exhibited high affinity for the blood–brain barrier choline transporter; and (=0.8 and 1.4μM, respectively) represent two of the most potent blood–brain barrier choline transporter ligands known.
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DOI：
10.1016/j.bmcl.2008.08.099
被引量：
年份：
2008
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