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<p>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 <b>5(a–r)</b> were synthesized, characterized by some spectroscopic techniques and evaluated for their potential as anti-Alzheimer agents. Among them, compound <b>5c</b>, bearing an <i>o</i>-fluoro phenyl group, showed multi-target inhibition with an IC₅₀ values of <b>78.07 ± 3.14 µM</b> acetylcholinesterase (<b>AChE</b>), 22.63 ± 2.81 µM butyrylcholinesterase (<b>BChE</b>) and 0.84 ± 0.01 µM monoamine oxidase A (<b>MAO-A</b>), showing higher inhibitory potential than the reference clorgyline with IC₅₀ value <b>66.20 ± 4.01 µM</b>. Other compounds, such as <b>5e</b>, <b>5&#xa0;g</b>, <b>5b</b> and <b>5q</b> 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 <b>5c</b> as a promising lead for multi-targeted AD therapy.</p>

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

  • 期刊论文

  • 出版模式：

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  • 发表日期：

    2025年12月13日

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  • Rahma Saeed,
  • Hafiza Zara Tariq,
  • Aiysha Althobaiti,
  • Nastaran Sadeghian,
  • Parham Taslimi,
  • Mariya Al-Rashida,
  • Talha Islam,
  • Hamdy Khamees Thabet,
  • Hina Aftab,
  • Halil Şenol,
  • Mubashir Ameen,
  • Jing Li,
  • Zahid Shafiq

摘要

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.