title: Synthesis of donepezil-based multifunctional agents for the treatment of Alzheimer's disease.
abstract: Amyloid beta (Aβ) and cholinesterase enzymes (AChE, BuChE) are important biological targets for the effective treatment of Alzheimer's disease. In this study, the aim was to synthesize new donepezil-like secondary amide compounds that display a potent inhibition of cholinesterases and Aβ with antioxidant and metal chelation abilities. All test compounds showed activities against both ChEs and β1-42 inhibition. The most encouraging compound, 20, is an AChE inhibitor with high anti-aggregation activity (55.3%). Based on the results, compound 20 may be a promising structure in further research for new anti-Alzheimer's agents.
authors.affiliation: Ataturk University, Faculty of Pharmacy, Department of Pharmaceutical Chemistry, 25240, Erzurum, Turkey. Electronic address: dadasozden@gmail.com.
authors.forename: Kadir Ozden
authors.initials: KO
authors.lastname: Yerdelen
authors.affiliation: Ataturk University, Faculty of Pharmacy, Department of Pharmaceutical Chemistry, 25240, Erzurum, Turkey.
authors.forename: Mehmet
authors.initials: M
authors.lastname: Koca
authors.affiliation: Ataturk University, Faculty of Pharmacy, Department of Organic Chemistry, 25240, Erzurum, Turkey.
authors.forename: Baris
authors.initials: B
authors.lastname: Anil
authors.affiliation: Ataturk University, Faculty of Pharmacy, Department of Pharmacognosy, 25240, Erzurum, Turkey.
authors.forename: Handan
authors.initials: H
authors.lastname: Sevindik
authors.affiliation: Ataturk University, Faculty of Pharmacy, Department of Pharmaceutical Chemistry, 25240, Erzurum, Turkey.
authors.forename: Zeynep
authors.initials: Z
authors.lastname: Kasap
authors.affiliation: Ataturk University, Faculty of Medicine, Department of Pharmacology, 25240, Erzurum, Turkey.
authors.forename: Zekai
authors.initials: Z
authors.lastname: Halici
authors.affiliation: Ataturk University, Faculty of Pharmacy, Department of Pharmaceutical Chemistry, 25240, Erzurum, Turkey.
authors.forename: Kubra
authors.initials: K
authors.lastname: Turkaydin
authors.affiliation: Ataturk University, Faculty of Pharmacy, Department of Pharmaceutical Chemistry, 25240, Erzurum, Turkey.
authors.forename: Gulsen
authors.initials: G
authors.lastname: Gunesacar
mesh_terms: D000544:Alzheimer Disease / Q000188:drug therapy*; D000577:Amides / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D016229:Amyloid beta-Peptides / Q000737:chemistry; D020134:Catalytic Domain; D002800:Cholinesterase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry; D000077265:Donepezil; D015195:Drug Design; D007189:Indans / Q000138:chemical synthesis* / Q000737:chemistry / Q000627:therapeutic use; D020128:Inhibitory Concentration 50; D008958:Models, Molecular; D010880:Piperidines / Q000138:chemical synthesis* / Q000737:chemistry / Q000627:therapeutic use; D013329:Structure-Activity Relationship
chemical_list: D000577:Amides; D016229:Amyloid beta-Peptides; D002800:Cholinesterase Inhibitors; D007189:Indans; D010880:Piperidines; D000077265:Donepezil
keywords: AChE; Alzheimer; Amyloid beta; BuChE; Donepezil