Structure-activity relationship of imidazo[1,2-a]pyridines as ligands for detecting beta-amyloid plaques in the brain.

@article{Zhuang2003StructureactivityRO,
  title={Structure-activity relationship of imidazo[1,2-a]pyridines as ligands for detecting beta-amyloid plaques in the brain.},
  author={Z P Zhuang and M. -P. Kung and A. D. Wilson and Chi-Wan Lee and Karl Ploessl and Catherine Hou and David M Holtzman and Hank F Kung},
  journal={Journal of medicinal chemistry},
  year={2003},
  volume={46 2},
  pages={237-43}
}
A series of novel beta-amyloid (A beta) aggregate-specific ligands, 2-(4'-dimethylaminophenyl)-6-iodoimidazo[1,2-a]pyridine, 16(IMPY), and its related derivatives were prepared. An in vitro binding study with preformed A beta aggregates showed that 16(IMPY) and its bromo derivative competed with binding of 2-(4'-dimethylaminophenyl)-6-iodobenzothiazole, [125I]7(TZDM), a known ligand for A beta aggregates, with high binding affinities (K(i) = 15 and 10 nM, respectively). In vitro autoradiography… CONTINUE READING

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