Carregant...
Fitxers
Tipus de document
ArticleVersió
Versió publicadaData de publicació
Llicència de publicació
Si us plau utilitzeu sempre aquest identificador per citar o enllaçar aquest document: https://hdl.handle.net/2445/194019
New cyclopentaquinoline and 3,5-dichlorobenzoic acid hybrids with neuroprotection against oxidative stress for the treatment of Alzheimer's disease
Títol de la revista
Director/Tutor
ISSN de la revista
Títol del volum
Recurs relacionat
Resum
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.
Matèries
Matèries (anglès)
Citació
Citació
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. New cyclopentaquinoline and 3,5-dichlorobenzoic acid hybrids with neuroprotection against oxidative stress for the treatment of Alzheimer's disease. _Journal of Enzyme Inhibition and Medicinal Chemistry_. 2023. Vol. 38, núm. 1. [consulta: 21 de gener de 2026]. ISSN: 1475-6366. [Disponible a: https://hdl.handle.net/2445/194019]