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

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 A?1-40. 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 A? plaques.

SUBMITTER: Zeng F

PROVIDER: S-EPMC4007799 | biostudies-other | 2010 May

REPOSITORIES: biostudies-other

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

Zeng Fanxing F Alagille David D Tamagnan Gilles D GD Ciliax Brian J BJ Levey Allan I AI Goodman Mark M MM

ACS medicinal chemistry letters 20100311 2

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 emissio ...[more]

PMID: 24900181

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