Cited by 105Alzheimer's disease research and treatmentsCholinesterase and Neurodegenerative DiseasesSynthesis and biological activity

Synthesis and biological evaluation of deferiprone-resveratrol hybrids as antioxidants, Aβ 1–42 aggregation inhibitors and metal-chelating agents for Alzheimer's disease

Xu, Ping, Zhang, Minkui, Sheng, Rong, Ma, Yongmin·2017·European Journal of Medicinal Chemistry

Abstract

A series of deferiprone-resveratrol hybrids have been designed and synthesized as multitarget-directed ligands (MTDLs) through merging the chelating moiety 3-hydroxypyridin-4-one into the structure of resveratrol, a natural antioxidant agent and β-amyloid peptide (Aβ) aggregation inhibitor. The in vitro biological evaluation revealed that most of these newly synthesized compounds exhibited good inhibitory activity against self-induced Aβ 1-42 aggregation, excellent antioxidant activity and potent metal chelating capability. Compounds 3i and 4f were identified as the most promising MTDLs with triple functions, possessing micromolar IC 50 values for Aβ 1-42 aggregation inhibition, greater 2,2'-azino-bis(3-ethylbenzthiazoline-6-sulfonic acid) (ABTS•+) scavenging activity than Trolox and similar pFe(III) values to that of deferiprone.

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Crossref · 10.1016/j.ejmech.2016.12.045

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  • Deferiprone is an iron chelating agent studied in phase 2 trials in participants with mild and prodromal Alzheimer disease.

    “Deferiprone is an iron chelating agent which is studied in phase 2 trials in participants with mild and prodromal AD.4,53”

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Authors
Xu, P., Zhang, M., Sheng, R., & Ma, Y.
Affiliations
  • Zhejiang Chinese Medical University (CN)
  • Zhejiang University (CN)
Corresponding author
  • Sheng, Rong
  • Ma, Yongmin
Venue
European Journal of Medicinal Chemistry
Publisher
Elsevier BV
Published
2017-02
Volume
127
Pages
174-186
ISSN
0223-5234 (ISSN-L)
OpenAlex
W2563664591
Cited by
92
References
36
Citations by year
2026: 3 · 2025: 7 · 2024: 6 · 2023: 10 · 2022: 11 · 2021: 16 · 2020: 11 · 2019: 9 · 2018: 13 · 2017: 6
FWCI
7.45
Type
journal article
Language
en
Open access
closed
Locations
  • European Journal of Medicinal Chemistry (publishedVersion)
  • PubMed (publishedVersion)
Funders
  • Zhejiang provincial Natural Science Foundation of China (LY17H300005)
  • Zhejiang Chinese Medical University (2015ZG15)
Topics
  • Health Sciences › Medicine › Physiology › Alzheimer's disease research and treatments
  • Health Sciences › Medicine › Pharmacology › Cholinesterase and Neurodegenerative Diseases
  • Physical Sciences › Chemistry › Organic Chemistry › Synthesis and biological activity
Keywords
multi-target-directed ligands, Alzheimer's disease, antioxidant activity, metal chelation, 3-hydroxypyridin-4-ones, resveratrol, ABTS radical scavenging, multi-target drugs
MeSH terms
Resveratrol, Deferiprone, Alzheimer Disease, Antioxidants, Chelating Agents, Copper, Iron, Peptide Fragments, Pyridones, Stilbenes, Structure-Activity Relationship, Drug Design, Amyloid beta-Peptides, Protein Structure, Secondary, Chemistry Techniques, Synthetic, Molecular Docking Simulation, Protein Aggregates

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