National Repository of Grey Literature 154 records found  1 - 10nextend  jump to record: Search took 0.00 seconds. 
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...
Monitoring of alkali-silica reaction
Doležal, Martin ; Kalina, Lukáš (referee) ; Opravil, Tomáš (advisor)
Due to the alkali-silica reaction (ASR), concrete structures are damaged, which can lead to the loss of their useful properties. For the reaction to take place, the presence of alkalis is required. During the work, the release of alkalis into the pore solution was monitored. During hydration pore solutions were taken, on the basis of calorimetric curves. In pore solutions the K+ a Na+ content was analyzed by ICP-OES. The result is graphs of the development of alkali content and their relationship to cement hydration. The danger of the alkali in tested samples for the course of the reaction is described here. The description of the alkali content and its development is important for understanding the course of ASR and proposing a viable solution to protect against this problem.
Metody měření hustoty mléčných výrobků
Doležal, Martin
This bachelor thesis deals with density of dairy products and measurement of it. The first part of the bachelor thesis describes the density and methods of its measuremen. The second part of the bachelor thesis describes the composition of milk and dairy products. In the experimental part of the bachelor thesis deals with the influence of temperature on the density of milk and dairy products. Milk with a fat content of 3.5 %, 1.5% and 0.5%, cream with a fat content of 12% and 31% and acidophilic milk were used. Densito 30 PX was used to measure density. As expected, the density dropped with increasing temperature.Formula clause:Prohlašuji, že jsem práci: Metody měření hustoty mléčných výrobků, vypracoval samostatně a veškeré použité prameny a informace uvádím v seznamu použité literatury. Souhlasím, aby moje práce byla zveřejněna v souladu s § 47b zákona č. 111/1998 Sb., o vysokých školách a o změně a doplnění dalších zákonů (zákon o vysokých školách), ve znění pozdějších předpisů, a v souladu s platnou Směrnicí o zveřejňování vysokoškolských závěrečných prací. Jsem si vědom/a, že se na moji práci vztahuje zákon č. 121/2000 Sb., autorský zákon, a že Mendelova univerzita v Brně má právo na uzavření licenční smlouvy a užití této práce jako školního díla podle § 60 odst. 1 autorského zákona. Dále se zavazuji, že před sepsáním licenční smlouvy o využití díla jinou osobou (subjektem) si vyžádám písemné stanovisko univerzity, že předmětná licenční smlouva není v rozporu s oprávněnými zájmy univerzity, a zavazuji se uhradit případný příspěvek na úhradu nákladů spojených se vznikem díla, a to až do jejich skutečné výše
Derivatives of pyrazinecarboxylic acid as potential antimycobacterial active drugs.
Bouz, Ghada Basem ; Doležal, Martin (advisor) ; Musiol, Robert (referee) ; Krátký, Martin (referee)
Charles University, Faculty of Pharmacy in Hradec Králové Department of Department of Pharmaceutical Chemistry and Pharmaceutical Analysis Candidate Ghada Bouz Supervisor Prof. PharmDr. Martin Doležal, Ph.D. Title of Doctoral Thesis Derivatives of Pyrazinecarboxylic Acid as Potential Antimycobacterial Active Drugs This doctoral thesis is focused on the design, synthesis, and in vitro antimicrobial evaluation of potentially active compounds structurally derived from the first line antitubercular, pyrazinamide. The introduction briefly highlights the serious issue of tuberculosis in the present time, along with the reasons behind the failure to eradicate this ancient infection. The lack of a proper animal model that can replicate tuberculosis in its latent and active form was discussed more in detail, where zebrafish (Danio rerio) was suggested as a novel animal model suitable for multi-research purposes connected to tuberculosis. A total of 112 compounds were synthesized and published as part of this doctoral work. They are divided into four main structural types, namely 3-(phenylcarbamoyl)pyrazine-2-carboxylic acids, 3- aminopyrazine-2-carboxamides, ureidopyrazines, and N-(pyrazin-2-yl)benzenesulfonamides. All prepared compounds were in vitro screened against five mycobacterial strains (with the...
Monitoring of basic pharmacokinetic parameters of acetylcholinesterase inhibitors used in the treatment of Alzheimer's disease
Krejčiová, Markéta ; Doležal, Martin (advisor) ; Vopršalová, Marie (referee)
Charles University in Prague Faculty of Pharmacy in Hradec Králové Department of Pharmaceutical Chemistry and Control of Pharmaceuticals Student: Markéta Krejčiová Supervisor: Prof. PharmDr. Martin Doležal, Ph.D. Supervisor specialist: Mjr. PharmDr. Jana Žďárová Karasová, Ph.D. Title of diploma thesis: Monitoring of basic pharmacokinetic parameters of acetylcholinesterase inhibitors used in the treatment of Alzheimer's disease Alzheimer's disease is a progressive irreversible neurodegenerative disorder that is globally associated with the most frequent cause of dementia. The pathophysiology of this illness is not fully understood yet. The commonly used treatment is still symptomatic, based on IAChE and memantine. Great attention is paid particularly to IAChEs and their derivatives, which arise from the basic structure of tacrine and 7-MEOTA. These two molecules were used as a reference for comparison with newly synthetized IAChE derivatives KB-36 and KB-38. Changes in plasma and brain tissue concentration levels were studied. The in vivo study was performed on rats (male, tribe Wistar). Equimolar doses were administered intramuscularly. Samples of plasma and brain tissue were evaluated by using HPLC techniques. The main aim was to determine the real concentration levels of all IAChE in both...
Toward new analogues of vitamin E: new potential inhibitors of 5-lipoxygenase
Štůsková, Martina ; Tůmová, Lenka (advisor) ; Doležal, Martin (referee)
Many studies highlighted the biological potential of vitamin E, especially tocotrienols (T3), a vitamin E subfamily, particularly in the field of cardiovascular diseases and chronic inflammation. A pharmacophore based virtual screening of these substances against various antiinflammatory targets showed that this class could be considered as potential inhibitors of 5- lipoxygenase, a key enzyme in the biosynthesis of chemoattractant and vasoactive leukotrienes. Consequently, this screening was confirmed by in vitro assays. However, usual natural sources of T3 provide complex mixtures involving particularly challenging purification processes. Thus, this work aims at designing and optimizing efficient semisynthesis towards pharmacologically relevant T3 derivatives were developed from δ- tocotrienol, the main T3 isolated from Bixa orellana seeds, a renewable and easily available vegetal source from tropical regions, analyzed mainly by HPLC chromatography. Verification of the most effective reaction conditions of semisynthesis and synthesis another potential inhibitors of 5-LOX based on tocotrienols' structure are the following aims of the work. During this study, the semisynthesis based on δ-tocotrienol was completely optimized and 3 new T3 derivatives were synthesized and fully characterized....
Commented translation of a text on science and technology
Doležal, Martin ; Smutný, Milan (referee) ; Krhutová, Milena (advisor)
Tato bakalářská práce se zabývá používáním technického jazyka v češtině i angličtině, v čem si jsou tyto jazyky podobné a v čem se naopak liší. Pro studování jazyků v elektrotechnice byl vybrán technicky zaměřený text k přeložení a poté byl přeložen do angličtiny. Po překladu byla provedena analýza jazyka, které se zaměřovala jak na lingvistické, tak extralingvistické vlastnosti, které jsou často specifické pro odborné texty. Tyto vlastnosti pokrývají širokou škálu lingvistických oborů, jako jsou například lexikologie, morfologie, stylistika, syntax, ale i extralingvistické záležitosti, jako třeba pragmatika. Analýza originálního a přeloženého textu odhalila spoustu rozdílů, jak malých, tak i velkých, které jsou výsledkem pokusu o přenos informace v jazyce, který je poměrně rozdílný oproti originálnímu jazyku.
Propargyltacrines - acetylcholinesterase inhibitors with anti-MAO activity
Nemčíková, Lenka ; Kučerová, Marta (advisor) ; Doležal, Martin (referee)
Charles University Faculty of Pharmacy in Hradec Králové Department of Pharmaceutical Chemistry and Pharmaceutical Analysis Student: Lenka Nemčíková Supervisor: PharmDr. Marta Kučerová, Ph.D. Title of Thesis: Propargyltacrines - acetylcholinesterase inhibitors with anti-MAO activity Alzheimer's disease (AD) is a serious neurodegenerative disorder that affects mainly aged people. Neurodegenerative disorders lead to dementia. However, dementia is not a part of normal aging. It is the result of pathologigal process. Alois Alzheimer was the first who described AD. The causes of this disease are not clear, however partial pathological mechanisms and the risk factors are known. There is no drug for casual treatment of AD. Nowadays, we can only slow down the symptoms or development of dementia by combining pharmacological and non-pharmacological techniques. Such approach could improve the quality of life of affected people. The treatment of AD involves acetylcholinesterase (AChE) inhibitors and N-methyl-D-aspartate receptor antagonist (NMDA). Donepezil, rivastigmine and galantamine belong to AChE inhibitors. Decrease in AChE activity leads to balance in acetylcholine transmission, which is disturbed in early stages of the disease. Tacrine was the first drug launched on the market for the treatment of...
Pyrazine derivatives as potential drugs V.
Mindlová, Alžběta ; Doležal, Martin (advisor) ; Kučerová, Marta (referee)
Charles University in Prague Faculty of Pharmacy in Hradec Králové Department of Pharmaceutical Chemistry and Drug Control Author: Alžběta Mindlová Supervisor: prof. PharmDr. Martin Doležal, Ph.D. Title of diploma thesis: Pyrazine Derivatives as Potential Drugs V This study deals with the issue of tuberculosis, which is a second leading cause of deaths after HIV from all infectious diseases worldwide. This is supported by an ever increasing number of mycobacteria, which is resistant to conventional antituberculotics. Because of grow of the multidrug-resistant tuberculosis, there is need for the development of new drugs in the therapy of this disease. The design of final compounds was based on the previously prepared pyrazine-2- carboxilic acid, which exerted antituberculotic activity. The object of study was to verify the effectiveness of N-(pyrazine-2-yl)benzamides created by an imaginary variation of the connecting bridge between the pyrazine and benzene ring. In the experimental part of the work the synthesis of twenty three substances derived from 2-aminopyrazin or 6-chlor-2- aminopyrazin is described. All products have been described by melting point, 1 H, 13 C NMR, IR spectroscopy and the elementary analysis. The substances were send for the biological evaluation, where were tested for...
Definition of the carbohydrate binding capacities of the novel enterotoxin LT-IIc
Juhás, Martin ; Doležal, Martin (advisor) ; Jirkovská, Anna (referee)
Diarrhoea as a disease is still the leading cause of malnutrition and a major cause of deaths in children under 5 years of age in the low-income countries. Additionally, it is the most common health problem associated with travelling to the developing countries. In all the mentioned cases, enterotoxigenic E. coli (ETEC) is one of the most frequent causes. ETEC is defined as a pathogenic strain of E. coli producing enterotoxins. So far, two types of enterotoxins have been identified: heat-stable (ST) and heat-labile (LT). LTs are further divided into two categories based on their relatedness with cholera toxin to type I (LT-I) and type II (LT-II). All of these enterotoxins have been found to bind to carbohydrate structures on glycosphingolipids by their respective B subunits, however, their binding patterns differ. While LT-I, LT-IIa and LT-IIb have been previously studied in terms of binding specificities, the newest LT-IIc was tested only on few commercially available ganglio-series gangliosides. In this thesis, the binding capabilities of this novel enterotoxin were re-examined by series of binding assays using more ganglio-series and some neolacto-series gangliosides as well as other glycolipids and glycoproteins, to establish the basics of the recognition pattern and to characterize the optimal...

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See also: similar author names
3 Doležal, Marek
5 Doležal, Michal
3 Doležal, Milan
4 Doležal, Miroslav
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