Resveratrol-maltol hybrids as multi-target-directed agents for Alzheimer’s disease
Bioorganic & Medicinal Chemistry
9 August 2018
Gang Cheng, Ping Xu, Minkui Zhang, Jing Chen, Rong Sheng, Yongmin Ma
https://doi.org/10.1016/j.bmc.2018.08.011
Abstract
The 3-hydroxypyran-4-one moiety (maltol) was incorporated into the structure of resveratrol to achieve a series of resveratrol-maltol hybrids (8a–8k) as novel multi-target-directed ligands (MTDLs). In vitro biological evaluation of the MTDLs revealed
these compounds to have a triple function, namely inhibition of self-induced Aβ1–42 aggregation, antioxidation, and metal chelating activity. Among all the evaluated MTDLs, compounds 8i and 8j showed the most promise, demonstrating micromolar IC50
values for Aβ1–42 aggregation inhibition, more potent ABTS+ scavenging activity than Trolox, and good metal chelating activities.
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