
Bioorganic and Medicinal Chemistry p. 5759 - 5765 (2018)
Update date:2022-07-29
Topics:
Cheng, Gang
Xu, Ping
Zhang, Minkui
Chen, Jing
Sheng, Rong
Ma, Yongmin
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[rad]+ scavenging activity than Trolox, and good metal chelating activities.
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