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Synthesis and evaluation of potential cholinesterases inhibitors
Houngbedji, Neto-Honorius ; Krátký, Martin (advisor) ; Kučerová, Marta (referee)
Charles University, Faculty of Pharmacy in Hradec Králové Department of Organic and Bioorganic Chemistry Author: Neto-Honorius Houngbedji Supervisor: PharmDr. Mgr. Martin Krátký, Ph.D. Title of diploma thesis: Synthesis and evaluation of potential inhibitors of cholinesterases During the last years, the number of patients affected by Alzheimer's disease has been constantly increasing. This disease, which burdens the patients as well as their milieu, requires a costly treatment, based on the use of acetylcholinesterase inhibitors currently. The theoretical part summarizes the contemporary knowledge about the pathology, epidemiology and therapy of Alzheimer's disease. This part also presents the results of previous research of salicylanilide-based cholinesterase inhibitors. The use of acetylcholinesterase inhibitors in the treatment of Alzheimer's disease led to the design of eight novel compounds (esters of salicylanilides and phosphorus acids) with inhibitory activity against cholinesterases. Thus, the experimental part of this diploma thesis consists in the synthesis, characterization and biological evaluation of the novel inhibitors. Finally, three new compounds were synthesized and evaluated successfully. Their inhibitory activities (IC50) were within the range of 48.13-66.13 µM against...
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Synthesis and evaluation of potential cholinesterases inhibitors
Houngbedji, Neto-Honorius ; Krátký, Martin (advisor) ; Kučerová, Marta (referee)
Charles University, Faculty of Pharmacy in Hradec Králové Department of Organic and Bioorganic Chemistry Author: Neto-Honorius Houngbedji Supervisor: PharmDr. Mgr. Martin Krátký, Ph.D. Title of diploma thesis: Synthesis and evaluation of potential inhibitors of cholinesterases During the last years, the number of patients affected by Alzheimer's disease has been constantly increasing. This disease, which burdens the patients as well as their milieu, requires a costly treatment, based on the use of acetylcholinesterase inhibitors currently. The theoretical part summarizes the contemporary knowledge about the pathology, epidemiology and therapy of Alzheimer's disease. This part also presents the results of previous research of salicylanilide-based cholinesterase inhibitors. The use of acetylcholinesterase inhibitors in the treatment of Alzheimer's disease led to the design of eight novel compounds (esters of salicylanilides and phosphorus acids) with inhibitory activity against cholinesterases. Thus, the experimental part of this diploma thesis consists in the synthesis, characterization and biological evaluation of the novel inhibitors. Finally, three new compounds were synthesized and evaluated successfully. Their inhibitory activities (IC50) were within the range of 48.13-66.13 µM against...
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