Multitarget-Directed Benzylideneindanone Derivatives: Anti-β-Amyloid (Aβ) Aggregation, Antioxidant, Metal Chelation, and Monoamine Oxidase B (MAO-B) Inhibition Properties against Alzheimer’s Disease

A novel series of benzylideneindanone derivatives were designed, synthesized, and evaluated as multitarget-directed ligands against Alzheimer’s disease. The in vitro studies showed that most of the molecules exhibited a significant ability to inhibit self-induced β-amyloid (Aβ_1–42) aggregation (10.5–80.1%, 20 μM) and MAO-B activity (IC₅₀ of 7.5–40.5 μM), to act as potential antioxidants (ORAC-FL value of 2.75–9.37), and to function as metal chelators. In particular, compound <b>41</b> had the greatest ability to inhibit Aβ_1–42 aggregation (80.1%), and MAO-B (IC₅₀ = 7.5 μM) was also an excellent antioxidant and metal chelator. Moreover, it is capable of inhibiting Cu­(II)-induced Aβ_1–42 aggregation and disassembling the well-structured Aβ fibrils. These results indicated that compound <b>41</b> is an excellent multifunctional agent for the treatment of AD

Additional file 1: of Safety, pharmacokinetics, metabolism and radiation dosimetry of 18F-tetrafluoroborate (18F-TFB) in healthy human subjects

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