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Author Notes:

To whom correspondence should be addressed. Tel: 404-727-9366. Fax: 404-727-3488. E-mail: mgoodma@emory.edu.

Subjects:

Keywords:

  • Imidazo[1,2-b]pyridazine
  • β-amyloid plaque
  • structure−activity relationship
  • positron emission tomography

Synthesis and In Vitro Evaluation of Imidazo[1,2-b]pyridazines as Ligands for ?-Amyloid Plaques

Tools:

Journal Title:

ACS Medicinal Chemistry Letters

Volume:

Volume 1, Number 2

Publisher:

, Pages 80-84

Type of Work:

Article | Post-print: After Peer Review

Abstract:

A series of imidazo[1,2-b]pyridazine derivatives were synthesized and evaluated for binding to amyloid plaques in vitro using synthetic aggregates of Aβ1−40. Binding affinities of these compounds were found to range from 11.0 to >1000 nM, depending on the various substitution patterns in the 6-position and 2-position. 2-(4′-Dimethylaminophenyl)-6-(methylthio)imidazo[1,2-b]pyridazine (4) showed high binding affinity (Ki = 11.0 nM) and might be useful for the development of novel positron emission tomography radiotracers for imaging Aβ plaques.

Copyright information:

© 2010 American Chemical Society

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