Dioxaborinine-styrylquinoline hybrids as multitarget small-molecule theranostic compounds against Alzheimer's disease

Novel push-pull conjugated molecules combining styrylquinoline and dioxaborinine units, as well as their β-dicarbonyl precursors were designed, synthesized and tested as multitarget theranostic agents against AD with promising results. In vitro experiments demonstrated favorable fluorescent properties for optical imaging; histological studies proved their excellent performance as selective amyloid-targeted optical probes and preliminary in vivo experiments confirmed their suitability as diagnostic agents for fluorescence imaging in AD mice with an intact skull, without the need of opening a cranial window. In terms of their therapeutic potential, in vitro experiments showed a good antiaggregating activity towards the two misfolded proteins involved in AD, amyloid β and tau protein. Overall, these compounds, and particularly the dioxaborinine derivatives, are promising multitarget theranostic candidates against Alzheimer's disease.