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Abstract In our study thirty-one new thiazole derivatives were designed and synthesized. Structure elucidation of the newly synthesized compounds was achieved via IR, 1H-NMR, 13C-NMR, mass spectroscopy and elemental analyses. All the new derivatives were evaluated biologically for their inhibitory capabilities against human acetylcholinesterase (hAChE), human butyrylcholinesterase (hBuChE) and β-amyloid (Aβ) aggregation, and investigated for their metal chelating potential as multi-target agents for the treatment of AD. Cytotoxicity studies were performed for the most potent AChE inhibitor and the most potent BuChE and Aβ, against human neuroblastoma SH-SY5Y and PC12 neuron cells. They proved non-cytotoxic at their active concentrations against hAChE or hBuChE. Both compounds showed a neuroprotective effect against Aβ25-35-induced-cytotoxicity in SH-SY5Y cells. Molecular docking studies were conducted for the most active compounds at the active sites of hAChE, hBuChE and Aβ1-42 using Autodock Vina as the docking engine. The docking results were in good agreement with the biological results. |