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

[摘要]：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 beta(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 beta plaques.

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