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LC-MS analysis of phase one biotransformation of K1277, a potential drug against Alzheimer's disease
Krchová, Lucie ; Štaud, František (advisor) ; Kučera, Radim (referee)
Charles University Faculty of Pharmacy in Hradec Králové Department of Pharmacology & Toxicology Student: Lucie Krchová Supervisor: Prof. PharmDr. František Štaud, Ph.D. Supervisor - Consultant: Mgr. et Mgr. Rafael Doležal, Ph.D. Title of diploma thesis: LC-MS analysis of phase one biotransformation of K1277, a potential drug against Alzheimer's disease. Alzheimer's disease belongs to the most common neurodegenerative diseases that several milions of people all around the world suffer from. There are few symptomatic drugs, which are able to reduce signs and symptoms of this type of dementia, however none of them is able to completely stop it. The diploma thesis is focused on a metabolomic study of compound K1277, synthesized as a combination of 6-chlortacrine and aminoacid tryptophan, which thanks to its properties belongs to promising potential drugs against Alzheimer's disease and which has not been published yet. The aim of this diploma thesis was to perform in vitro metabolomic screening of the compound K1277 using human liver microsomes focusing on qualitative and quantitative analysis. As intermediate aims of the thesis, necessary conditions for sufficient biotransformation of compound K1277 were investigated, quantity of metabolised compound K1277, identifications of particular metabolites...
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LC-MS analysis of phase one biotransformation of K1277, a potential drug against Alzheimer's disease
Krchová, Lucie ; Štaud, František (advisor) ; Kučera, Radim (referee)
Charles University Faculty of Pharmacy in Hradec Králové Department of Pharmacology & Toxicology Student: Lucie Krchová Supervisor: Prof. PharmDr. František Štaud, Ph.D. Supervisor - Consultant: Mgr. et Mgr. Rafael Doležal, Ph.D. Title of diploma thesis: LC-MS analysis of phase one biotransformation of K1277, a potential drug against Alzheimer's disease. Alzheimer's disease belongs to the most common neurodegenerative diseases that several milions of people all around the world suffer from. There are few symptomatic drugs, which are able to reduce signs and symptoms of this type of dementia, however none of them is able to completely stop it. The diploma thesis is focused on a metabolomic study of compound K1277, synthesized as a combination of 6-chlortacrine and aminoacid tryptophan, which thanks to its properties belongs to promising potential drugs against Alzheimer's disease and which has not been published yet. The aim of this diploma thesis was to perform in vitro metabolomic screening of the compound K1277 using human liver microsomes focusing on qualitative and quantitative analysis. As intermediate aims of the thesis, necessary conditions for sufficient biotransformation of compound K1277 were investigated, quantity of metabolised compound K1277, identifications of particular metabolites...
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