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Preparation of phenyl derived benzothiazoles as potential ABAD modulators
Chřibek, Matěj ; Doležal, Martin (advisor) ; Kučerová, Marta (referee)
Charles University in Prague Faculty of Pharmacy in Hradec Králové Department of Pharmaceutical Chemistry and Drug Control Student: Matěj Chřibek Supervisor: prof. PharmDr. Martin Doležal, Ph.D. Title of Thesis: Preparation of phenyl derived benzothiazoles as potential ABAD mo- dulators Alzheimer's disease (AD) is neurodegenerative disease, which is characterized by progressive cognitive decline. Characteristic symptoms are memory loss, change of behaviour and personality. The pathological hallmarks of AD are senile plaques and neurofibrillary tangles of hyperphosphorylated τ protein. Currently there is no causal treatment, because the aetiology stays unexplained, despite of intensive research. Nowadays, the hypothesis assumes that soluble form of amyloid-β (Aβ) is asso- ciated with toxic effects inside the cells, among others in mitochondria. There are many intracellular proteins, which interact with Aβ, such as amyloid binding alcohol dehydrogenase (ABAD). Interaction Aβ-ABAD with consequent alteration of ABAD function has been shown to cause mitochondrial dysfunction, consequently leading to the cell death. Therefore, inhibition of Aβ-ABAD along with ABAD inhibition seems as a potential pharmacological target. 1 The aim of this thesis was to synthesize substituted benzothiazole ureas as...
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Preparation of phenyl derived benzothiazoles as potential ABAD modulators
Chřibek, Matěj ; Doležal, Martin (advisor) ; Kučerová, Marta (referee)
Charles University in Prague Faculty of Pharmacy in Hradec Králové Department of Pharmaceutical Chemistry and Drug Control Student: Matěj Chřibek Supervisor: prof. PharmDr. Martin Doležal, Ph.D. Title of Thesis: Preparation of phenyl derived benzothiazoles as potential ABAD mo- dulators Alzheimer's disease (AD) is neurodegenerative disease, which is characterized by progressive cognitive decline. Characteristic symptoms are memory loss, change of behaviour and personality. The pathological hallmarks of AD are senile plaques and neurofibrillary tangles of hyperphosphorylated τ protein. Currently there is no causal treatment, because the aetiology stays unexplained, despite of intensive research. Nowadays, the hypothesis assumes that soluble form of amyloid-β (Aβ) is asso- ciated with toxic effects inside the cells, among others in mitochondria. There are many intracellular proteins, which interact with Aβ, such as amyloid binding alcohol dehydrogenase (ABAD). Interaction Aβ-ABAD with consequent alteration of ABAD function has been shown to cause mitochondrial dysfunction, consequently leading to the cell death. Therefore, inhibition of Aβ-ABAD along with ABAD inhibition seems as a potential pharmacological target. 1 The aim of this thesis was to synthesize substituted benzothiazole ureas as...
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Preparation of phenyl derived benzothiazoles as potential ABAD modulators
Chřibek, Matěj ; Doležal, Martin (advisor) ; Kučerová, Marta (referee)
Charles University in Prague Faculty of Pharmacy in Hradec Králové Department of Pharmaceutical Chemistry and Drug Control Student: Matěj Chřibek Supervisor: prof. PharmDr. Martin Doležal, Ph.D. Title of Thesis: Preparation of phenyl derived benzothiazoles as potential ABAD mo- dulators Alzheimer's disease (AD) is neurodegenerative disease, which is characterized by progressive cognitive decline. Characteristic symptoms are memory loss, change of behaviour and personality. The pathological hallmarks of AD are senile plaques and neurofibrillary tangles of hyperphosphorylated τ protein. Currently there is no causal treatment, because the aetiology stays unexplained, despite of intensive research. Nowadays, the hypothesis assumes that soluble form of amyloid-β (Aβ) is asso- ciated with toxic effects inside the cells, among others in mitochondria. There are many intracellular proteins, which interact with Aβ, such as amyloid binding alcohol dehydrogenase (ABAD). Interaction Aβ-ABAD with consequent alteration of ABAD function has been shown to cause mitochondrial dysfunction, consequently leading to the cell death. Therefore, inhibition of Aβ-ABAD along with ABAD inhibition seems as a potential pharmacological target. 1 The aim of this thesis was to synthesize substituted benzothiazole ureas as...
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