Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10596022 | Bioorganic & Medicinal Chemistry Letters | 2013 | 6 Pages |
Abstract
To develop new drugs for treatment of Alzheimer's disease, a group of Nâ²-2-(4-Benzylpiperidin-/piperazin-1-yl)acylhydrazones was designed, synthesized and tested for their ability to inhibit acetylcholinesterase, butyrylcholinesterase and aggregation of amyloid beta peptides (1-40, 1-42 and 1-40_1-42). The enzyme inhibition assay results indicated that compounds moderately inhibit both acetylcholinesterase and butyrylcholinesterase. β-Amyloid aggregation results showed that all compounds exhibited remarkable Aβ fibril aggregation inhibition activity with a nearly similar potential as the reference compound rifampicin, which makes them promising anti-Alzheimer drug candidates. Docking experiments were carried out with the aim to understand the interactions of the most active compounds with the active site of the cholinesterase enzymes.
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Authors
Eda Ãzturan Ãzer, Oya Unsal Tan, Keriman Ozadali, Tuba Küçükkılınç, Ayla Balkan, Gülberk Uçar,