New 1,2,4-oxadiazole derivatives as potential multifunctional agents for the treatment of Alzheimer's disease: design, synthesis, and biological evaluation.

ABSTRACT: A series of new 1,2,4-oxadiazole-based derivatives were synthesized and evaluated for their anti-AD potential. The results revealed that eleven compounds (1b, 2a-c, 3b, 4a-c, and 5a-c) exhibited excellent inhibitory potential against AChE, with IC₅₀ values ranging from 0.00098 to 0.07920 µM. Their potency was 1.55 to 125.47 times higher than that of donepezil (IC₅₀ = 0.12297 µM). In contrast, the newly synthesized oxadiazole derivatives with IC₅₀ values in the range of 16.64-70.82 µM exhibited less selectivity towards BuChE when compared to rivastigmine (IC₅₀ = 5.88 µM). Moreover, oxadiazole derivative 2c (IC₅₀ = 463.85 µM) was more potent antioxidant than quercetin (IC₅₀ = 491.23 µM). Compounds 3b (IC₅₀ = 536.83

SUBMITTER: Ayoup MS 

PROVIDER: S-EPMC11246588 | biostudies-literature | 2024 Jul

REPOSITORIES: biostudies-literature