Bioorganic and Medicinal Chemistry p. 5917 - 5928 (2017)
Update date:2022-08-11
Topics:
Yang, Hua-Li
Cai, Pei
Liu, Qiao-Hong
Yang, Xue-Lian
Fang, Si-Qiang
Tang, Yan-Wei
Wang, Cheng
Wang, Xiao-Bing
Kong, Ling-Yi
A series of salicyladimine derivatives were designed, synthesized and evaluated as multi-target-directed ligands for the treatment of Alzheimer's disease (AD). Biological activity results demonstrated that some derivatives possessed significant inhibitory activities against amyloid-β (Aβ) aggregation and human monoamine oxidase B (hMAO-B) as well as remarkable antioxidant effects and low cell toxicity. The optimal compound, 5, exhibited excellent potency for inhibition of self-induced Aβ1–42 aggregation (91.3 ± 2.1%, 25 μM), inhibition of hMAO-B (IC50, 1.73 ± 0.39 μM), antioxidant effects (43.4 ± 2.6 μM of IC50 by DPPH method, 0.67 ± 0.06 trolox equivalent by ABTS method), metal chelation and BBB penetration. Furthermore, compound 5 had neuroprotective effects against ROS generation, H2O2-induced apoptosis, 6-OHDA-induced cell injury, and a significant in vitro anti-inflammatory activity. Collectively, these findings highlighted that compound 5 was a potential balanced multifunctional neuroprotective agent for the development of anti-AD drugs.
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