| Summary: | Charles University in Prague Faculty of Pharmacy in Hradec Králové Department of Biological and Medical Sciences Candidate: Bc. Lenka Pulkrábková Supervisor: PharmDr. Miroslav Kovařík, Ph.D. Consultant: Mgr. Martina Hrabinová Title of diploma thesis: A comparison of tacrine - phenothiazine derivatives in the efficacy of cholinesterase inhibition Alzheimer's disease (AD) is a progressive fatal neurodegenerative disorder and the most common type of dementia. It is manifested by a variety of neuropsychiatric symptoms such as memory loss, social skills etc. Ethiology and pathogenesis of the disease has a multifactorial character and is not well known. Among the major pathological features belong: presence of neuronal loss, especially loss of cholinergic neurons, extracellular amyloid plaques, intracellular aggregates of hyperphosphorylated tau protein, oxidative stress etc. As AD is influenced by multiple factors, the main strategy in treatment is intervention multiple targets in the brain as well. Such drugs are denoted as multi-target- directed ligands (MTDLs) and they affect different molecular abnormalities of AD. The aim of this diploma thesis was the evaluation of the ability of tacrine- phenothiazine derivatives to inhibit cholinesterases (AChE, BChE). Derivatives with two to five carbons...
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