Synthesis and inhibitory activity of novel N-phenethylpiperidinehydrazide hydrazones against acetylcholinesterase, butyrylcholinesterase, and β-Amyloid (1–42) as potential anti-Alzheimer agents
Makaleler > Tam Makale · 2026
Yazarlar: Sülünay PARLAR ÇOŞKUN, Vildan ALPTÜZÜN
Bioorganic and Medicinal Chemistry Reports, Uluslararası, 2026, cilt 9
Özet
Novel N-phenethylpiperidine-hydrazide hydrazones were synthesized and evaluated for their inhibitory activities against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), with the most active compounds additionally assessed for their in vitro inhibition of ?-amyloid 42 (A?42) self-aggregation. The synthesized compounds were purified and structurally characterized using FT-IR, ¹H-NMR,13C-NMR, ESI-MS spectroscopy, and elemental analysis. All compounds exhibited inhibitory activity against AChE with IC50 values ranging from 6.32 to 8.24 µM, while some compounds showed moderate inhibition of BChE enzyme. Compound 3g (IC50= 6.32 ± 0.27 µM) and 3i (IC50= 6.32 ± 0.25 µM) showed the highest AChE inhibition, whereas compound 3a exhibited the highest BChE inhibition (IC50= 8.27 ± 0.34 µM). The most potent compounds were further tested for A?42 self-aggregation inhibition, demonstrating significant inhibitory effects with up to 72.95% inhibition at 100 µM. These results suggest that N-phenethylpiperidine-hydrazide hydrazones may serve as promising multi-target ligands for the treatment of AD.