ArticleScientific reports2025
Design, synthesis, and multi-target evaluation of 4-phenyl quinoline-8-sulfonate thiosemicarbazones as potential anti-Alzheimer agents.
Article in Scientific reports, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 3 papers.
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3 citing papers in PubMed.
- QSAR-ML- and Metadynamics-Guided Design of Symmetrical Bis-Indanones to Overcome Mutational Anchor Loss in Acetylcholinesterase.Pharmaceuticals (Basel, Switzerland) · 2026Article
- Development of coumarin-sulfonate scaffolds for cholinesterase inhibition: experimental and computational studies toward Alzheimer's disease therapy.RSC advances · 2026Article
- Dual-Site Acetylcholinesterase Inhibition and Multiscale Stability of Fused Quinoline Sulfonamides: A Chemoinformatic GA-MLR and Molecular Dynamics Study.International journal of molecular sciences · 2026Article
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13 authors.
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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.
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