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An efficient electrolyte‐triggered trifluoromethylation and halogenation at C5 position of 8‐aminoquinoline derivatives was developed, affording the C−H functionalization products in moderate to excellent yields. Furthermore, the mild and green reactions had lower energy consumption and shorter times. Most importantly, both transition‐metal catalysts and oxidants were avoided.

Based on the multitarget-directed ligands (MTDLs) strategy, a series of chromone-hydroxypyridinone hybrids were designed, synthesised, and evaluated as potential multimodal anti-AD ligands. Prospective iron-chelating effects and favourable monoamine oxidase B (MAO-B) inhibitory activities were observed for most of the compounds. Pharmacological assays led to the identification of compound 17d , which exhibited favourable iron-chelating potential (pFe 3+ = 18.52) and selective h MAO-B inhibitory activity (IC 50 = 67.02 ± 4.3 nM, SI = 11). Docking simulation showed that 17d occupied both the substrate and the entrance cavity of MAO-B, and established several key interactions with the pocket residues. Moreover, 17d was determined to cross the blood–brain barrier (BBB), and can significantly ameliorate scopolamine-induced cognitive impairment in AD mice. Despite its undesired pharmacokinetic property, 17d remains a promising multifaceted agent that is worth further investigation.

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