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2000
Volume 33, Issue 5
  • ISSN: 0929-8673
  • E-ISSN: 1875-533X
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Abstract

Introduction

Dyshomeostasis of Cu2+ and abnormal interactions between Cu2+ and β Amyloid peptide (Aβ) can promote Aβ aggregation and oxidative stress, which are considered to trigger Alzheimer’s Disease (AD). Metal chelating therapy is a promising approach for the treatment of AD.

Methods

In this study, 2-(2-hydroxyphenyl)benzazoles were synthesized microwave irradiation promotion. Chelators inhibiting Cu2+-induced Aβ aggregation were determined through turbidity assay and BCA protein assay, while anti-oxidants were detected HRP/Amplex red assay and fluorescent probe of DCFH-DA. Cell viability was measured by MTT assay.

Results

The bio-activity for inhibiting Cu2+ induced-Aβ aggregation of chelators S-1, S-3, S-4, S-5, S-7, S-10, N-5, N-9, N-10 O-2, O-4, X-N-2 was better than that of CQ. The ability of the chelators (S-1, S-10, O-2, O-5, N-9, and X-N-2) to decrease the level of ROS in Aβ+Cu2+ treated SH-SY5Y cells was better than that of CQ. The ability to attenuate Aβ-mediated cytotoxicity in SH-SY5Y cells of S-10 (O-2, O-5, and N-9) was better than that of CQ.

Conclusion

After the evolution of the bio-activities for the treatment of AD , it was found that 4 chelators (S-10, O-2, O-5, and N-9) exhibited better bio-activities than CQ in all aspects.

© 2026 The Author(s). Published by Bentham Science Publishers.
This is an open access article published under CC BY 4.0 https://creativecommons.org/licenses/by/4.0/legalcode
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Highly Efficient and Eco-friendly Synthesis and Bio-activities of 1,3-benzazoles as Cu (II) Chelators in Alzheimer’s Disease Therapy
Curr. Med. Chem. 33, 1004 (2026); https://doi.org/10.2174/0109298673371011250612094752
/content/journals/cmc/10.2174/0109298673371011250612094752
/content/journals/cmc/10.2174/0109298673371011250612094752
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  • Article Type:     Research Article
Keyword(s): 2-substituted-1,3-benzazole; amyloid β; antioxidant; copper ion; microwave irradiation; Synthesis

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