Bis-azaaromatic quaternary ammonium salts as ligands for the blood-brain barrier choline transporter

Guangrong Zheng; Zhenfa Zhang; Paul R. Lockman; Werner J. Geldenhuys; David D. Allen; Linda P. Dwoskin; Peter A. Crooks

doi:10.1016/j.bmcl.2010.04.098

Bis-azaaromatic quaternary ammonium salts as ligands for the blood-brain barrier choline transporter

Guangrong Zheng, Zhenfa Zhang, Paul R. Lockman, Werner J. Geldenhuys, David D. Allen, Linda P. Dwoskin, Peter A. Crooks

Research output: Contribution to journal › Article › peer-review

10 Scopus citations

Abstract

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.

Original language	English
Pages (from-to)	3208-3210
Number of pages	3
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	20
Issue number	11
DOIs	https://doi.org/10.1016/j.bmcl.2010.04.098
State	Published - Jun 1 2010

Bibliographical note

Funding Information:
This work was supported by the National Institute of Health foundation ( U19 DA017548 ).

Keywords

Bis-quaternary ammonium salts
Blood-brain barrier
Choline transporter

ASJC Scopus subject areas

Biochemistry
Molecular Medicine
Molecular Biology
Pharmaceutical Science
Drug Discovery
Clinical Biochemistry
Organic Chemistry

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10.1016/j.bmcl.2010.04.098

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title = "Bis-azaaromatic quaternary ammonium salts as ligands for the blood-brain barrier choline transporter",

abstract = "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.",

keywords = "Bis-quaternary ammonium salts, Blood-brain barrier, Choline transporter",

author = "Guangrong Zheng and Zhenfa Zhang and Lockman, {Paul R.} and Geldenhuys, {Werner J.} and Allen, {David D.} and Dwoskin, {Linda P.} and Crooks, {Peter A.}",

note = "Funding Information: This work was supported by the National Institute of Health foundation ( U19 DA017548 ).",

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AU - Zheng, Guangrong

AU - Zhang, Zhenfa

AU - Lockman, Paul R.

AU - Geldenhuys, Werner J.

AU - Allen, David D.

AU - Dwoskin, Linda P.

AU - Crooks, Peter A.

N1 - Funding Information: This work was supported by the National Institute of Health foundation ( U19 DA017548 ).

PY - 2010/6/1

Y1 - 2010/6/1

N2 - 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.

AB - 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.

KW - Bis-quaternary ammonium salts

KW - Blood-brain barrier

KW - Choline transporter

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JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

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ER -

Bis-azaaromatic quaternary ammonium salts as ligands for the blood-brain barrier choline transporter

Abstract

Bibliographical note

Keywords

ASJC Scopus subject areas

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