Synthesis of Biphenyltrienes as Probes for β-Amyloid Plaques

Zhi-Ping Zhuang, Mei-Ping Kung, and Hank F. Kung*
Departments of Radiology, and Pharmacology, University of Pennsylvania, Room 305, 3700 Market Street, Philadelphia, Pennsylvania 19104
J. Med. Chem., 2006, 49 (9), pp 2841–2844
DOI: 10.1021/jm051020k
Publication Date (Web): March 29, 2006
Copyright © 2006 American Chemical Society

 Department of Radiology.

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*

 Corresponding author. Tel:  (215) 662-3096. Fax:  (215) 349-5035. E-mail:kunghf@sunmac.spect.upenn.edu.

,

 Department of Pharmacology.

Abstract

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We report a series of p-hydroxy-, p-amino-, p-monomethylamino-, and p-monofluoroethylamino-substituted biphenyltrienes that displayed high binding affinities to β-amyloid plaques. In an in vitro binding assay using postmortem brain homogenates of Alzheimer's patients and [125I]9, the triene compounds showed excellent binding affinities. When labeled with suitable radionuclides, they are useful as in vivo imaging agents for detecting Aβ plaques in the brains of Alzheimer's patients.

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History

  • Published In Issue May 04, 2006
  • Received October 11, 2005

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