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Title: New cyclopentaquinoline and 3,5-dichlorobenzoic acid hybrids with neuroprotection against oxidative stress for the treatment of Alzheimer's disease
Author: Czarnecka, Kamila
Malgorzata, Girek
Krecisz, Pawel
Skibinski, Robert
Latka, Kamil
Jonczyk, Jakub
Bajda, Marek
Szymczyk, Piotr
Galita, Grzegorz
Kabzinski, Jacek
Majesterek, Ireneusz
Espargaró Colomé, Alba
Sabaté Lagunas, Raimon
Szymanski, Pawel
Keywords: Malaltia d'Alzheimer
Química farmacèutica
Alzheimer's disease
Pharmaceutical chemistry
Issue Date: 11-Jan-2023
Publisher: Taylor and Francis
Abstract: Alzheimer's disease (AD) is a progressive neurodegenerative brain disease. Thus, drugs including donepezil, rivastigmine, and galantamine are not entirely effective in the treatment of this multifactorial disease. The present study evaluates eight derivatives (3a-3h) as candidates with stronger anti-AD potential but with less side effects. Reactive oxygen species (ROS) assays were used to assess oxidative stress which involve in the neurodegeneration. The neuroprotective properties of 3e against oxidative stress were done in three experiments using MTT test. The anti-AD potential was determined based on their anticholinesterase inhibition ability, determined using Ellman's method, Aβ aggregation potential according to thioflavin (Th) fluorescence assay, and their antioxidative and anti-inflammatory activities. Compound 3e exhibited moderate cholinesterase inhibition activity (AChE, IC50 = 0.131 µM; BuChE, IC50 = 0.116 µM; SI = 1.13), significant inhibition of Aβ(1-42) aggregation (55.7%, at 5 µM) and acceptable neuroprotective activity. Extensive analysis of in vitro and in vivo assays indicates that new cyclopentaquinoline derivatives offer promise as candidates for new anti-AD drugs.
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It is part of: Journal of Enzyme Inhibition and Medicinal Chemistry, 2023, vol. 38, num. 1
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ISSN: 1475-6366
Appears in Collections:Articles publicats en revistes (Farmàcia, Tecnologia Farmacèutica i Fisicoquímica)

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