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  3. Design, synthesis, and multi-target evaluation of 4-phenyl quinoline-8-sulfonate thiosemicarbazones as potential anti-Alzheimer agents

Design, synthesis, and multi-target evaluation of 4-phenyl quinoline-8-sulfonate thiosemicarbazones as potential anti-Alzheimer agents

  • Sci Rep. 2025 Dec 13;15(1):44212. doi: 10.1038/s41598-025-32012-y.
Rahma Saeed 1,  Hafiza Zara Tariq 2,  Aiysha Althobaiti 3,  Nastaran Sadeghian 4,  Parham Taslimi 4,  Mariya Al-Rashida 5,  Talha Islam 5,  Hamdy Khamees Thabet 6,  Hina Aftab 1,  Halil Şenol 7,  Mubashir Ameen 8,  Jing Li 2,  Zahid Shafiq 9
Affiliations

Affiliations

  • 1 Institute of Chemical Sciences, Bahauddin Zakariya University, Multan, 60800, Pakistan.
  • 2 School of Chemistry, Xi'an Jiaotong University, Xianning West Road, Xi'an, 710049, China.
  • 3 Department of Biochemistry, College of Medicine, Taif University, P.O. Box 11099, Taif, 21944, Saudi Arabia.
  • 4 Department of Biotechnology, Faculty of Science, Bartin University, 74110, Bartin, Turkey.
  • 5 Department of Chemistry, Forman Christian College (A Chartered University), Lahore, Pakistan.
  • 6 Center for Scientific Research and Entrepreneurship, Northern Border University, 73213, Arar, Saudi Arabia.
  • 7 Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Bezmialem Vakif University, 34093, Fatih, Istanbul, Turkey.
  • 8 Faculty of Pharmacy, Bahauddin Zakariya University, Multan, 60800, Pakistan.
  • 9 Institute of Chemical Sciences, Bahauddin Zakariya University, Multan, 60800, Pakistan. zahidshafiq@bzu.edu.pk.
PMID: 41390681 DOI: 10.1038/s41598-025-32012-y
Abstract

Alzheimer’s disease (AD) is a progressive neurodegenerative disorder marked by cognitive and memory decline. A novel series of 4-phenyl-quinoline-8-sulfonate-based thiosemicarbazones 5(a–r) were synthesized, characterized by some spectroscopic techniques and evaluated for their potential as anti-Alzheimer agents. Among them, compound 5c, bearing an o-fluoro phenyl group, showed multi-target inhibition with an IC₅₀ values of 78.07 ± 3.14 µM acetylcholinesterase (AChE), 22.63 ± 2.81 µM butyrylcholinesterase (BChE) and 0.84 ± 0.01 µM Monoamine Oxidase A (MAO-A), showing higher inhibitory potential than the reference clorgyline with IC₅₀ value 66.20 ± 4.01 µM. Other compounds, such as 5e, 5 g, 5b and 5q also exhibited significant inhibition across targets. Molecular docking confirmed strong binding interactions, particularly with the catalytic sites of AChE, BChE and MAO-A. These findings highlight 5c as a promising lead for multi-targeted AD therapy.

Supplementary Information: The online version contains supplementary material available at 10.1038/s41598-025-32012-y.

Keywords

Multi-target-directed ligands; Neurodegenerative disorders; Quinoline-8-sulfonate; Thiosemicarbazones.

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