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This publication is protected and can be accessed only from certain IPs.

Title: Synthesis and characterization of novel multifunctional ligands aiming at symptoms and causes of Alzheimer's disease


The research described in the thesis includes the design of new multifunctional compounds with potential application in the therapy of Alzheimer's disease, their synthesis, spectra characteristics and analysis of results of in vitro and in silico tests. The first group of ligands are beta-secretase and cholinesterase inhibitors with anti-aggregating properties against amyloid beta (Aβ) and tau protein, while the second group comprises compounds combining 5-HT6 receptor antagonism with cholinesterase inhibitory activity. Structural modifications aimed at optimization of activity towards biological targets of interest and - in the case of the second group - improvement of physicochemical parameters. The compounds were synthesized using specially developed synthetic routes, and their biological activity was assessed in the following assays: Ellman's (cholinesterase inhibition), FRET-based (inhibition of betasecretase), thioflavin T / S in vitro and in cellulo (Aβ and tau aggregation), FRAP and ABTS (antioxidant properties) and radio ligand binding assay. The analysis of the obtained results allowed the identification of a number of new, compounds with a multidirectional mechanism of action, which are an excellent starting point for further research on the application of multifunctional ligands m the treatment of Alzheimer's disease.

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2 - studia doktoranckie

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Rada Dyscypliny Nauki farmaceutyczne


Więckowska, Anna

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eng; pol

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tylko w bibliotece

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Last modified:

Mar 25, 2024

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Jan 20, 2022

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Edition name Date
ZB-132232 Mar 25, 2024


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