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Synthesis and biological evaluation of novel tacrine-tryptophan derivatives
 Jarošová, Michaela ; Opletalová, Veronika (advisor) ; Zitko, Jan (referee)
Charles University in Prague Faculty of Pharmacy in Hradec Kralove Department of Pharmaceutical Chemistry and Drug Control Student: Michaela Jarošová Supervisor: Assoc. Prof. RNDr. Veronika Opletalová, Ph.D. Consultant: PharmDr. Jan Korábečný, Ph.D. Title of thesis: Study and biological evaluation of new tacrine-tryptophan derivatives Alzheimer's disease (AD) is a chronic neurodegenerative disease with characteristic histopathological changes in the brain. It is the most common cause of dementia. There is about 7.4 million people affected by AD in Europe today. In connection with aging of the population a significant increase of patients affected by the disease can be expected in the coming years. The cause of neural tissue damage is aggregated amyloid β (Aβ), which disrupts neurons by creating glial hem with consequent inflammatory processes. Hyperphosphorylated τ-protein causes neuronal damage intracellularly by forming so-called neurofibrillary tangles. This leads to macroscopically visible brain atrophy and loss of neurons. Current AD pharmacotherapy is based on influencing the cholinergic system. Acetylcholinesterase inhibitors (AChEIs) - rivastigmine, donepezil and galanthamine are used for this purpose. Memantine, antagonist of N-methyl-D-aspartate receptors (NMDA) has been approved for the...
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