Bis-azaaromatic quaternary ammonium salts as ligands for the blood-brain barrier choline transporter
Creator
Zheng G R; Zhang Z F; Lockman P R; Geldenhuys W J; Allen D D; Dwoskin L P; Crooks P A
Publisher
Bioorganic & Medicinal Chemistry Letters
Date
2010
2010-06
Description
A series of bis-azaaromatic quaternary ammonium compounds containing flexible polymethylenic linkers as well as conformationally restricted linkers were evaluated for their affinity for the blood-brain barrier choline transporter (BBB-ChT). The preliminary structure-activity relationships obtained from this study suggest that incorporating a linear, conformationally restricted linker into the molecule improves affinity for the BBB-ChT. (C) 2010 Elsevier Ltd. All rights reserved.