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

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 (K i = 11.0 nM) and might be useful for the development of novel positron emission tomography radiotracers for imaging Aβ plaques.
AuthorsFanxing Zeng, David Alagille, Gilles D Tamagnan, Brian J Ciliax, Allan I Levey, Mark M Goodman
JournalACS medicinal chemistry letters (ACS Med Chem Lett) Vol. 1 Issue 2 Pg. 80-4 (May 13 2010) ISSN: 1948-5875 [Electronic] United States
PMID24900181 (Publication Type: Journal Article)

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