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- W4313255487 abstract "Here, we have designed and synthesized a series of melatonin-alkylbenzylamine hybrids as multitarget agents for the treatment of Alzheimer's disease (AD). Most of them exhibited a potent multifunctional profile involving cholinesterase inhibition and antioxidant effects. Among these compounds, compound 5 was most the potent antioxidant (ORAC = 5.13) and also an excellent selective inhibitor of BuChE (huBuChE IC50 = 1.20 μM, huAChE IC50 = 177.49 μM, SI = 147.91). Moreover, kinetic study indicated compound 5 was a mixed-type inhibitor for huBuChE. Furthermore, it could induce expression of the Nrf2 as well as its downstream markers at the protein level in cells. More importantly, compound 5 display no acute toxicity in mice at doses up to 2500 mg/kg. And we found compound 5 could improve memory function of scopolamine-induced amnesia mice. These results highlighted compound 5 as a possible hit molecule for further investigation of new anti-AD drugs." @default.
- W4313255487 created "2023-01-06" @default.
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- W4313255487 date "2023-01-01" @default.
- W4313255487 modified "2023-09-30" @default.
- W4313255487 title "Dual functional antioxidant and butyrylcholinesterase inhibitors for the treatment of Alzheimer’s disease: Design, synthesis and evaluation of novel melatonin-alkylbenzylamine hybrids" @default.
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- W4313255487 doi "https://doi.org/10.1016/j.bmc.2022.117146" @default.
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