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Terpyridine derivatives: preparation and complexation properties
Vitvarová, Tereza ; Svoboda, Jan (advisor) ; Sedláček, Jan (referee)
In this thesis we report synthesis of chosen terpyridine derivatives and their availability to make a complex with Zinc (II) ions and Iron (II) ions. These complexes were characterised and we studied their suitability to build supramolecular materials. Iron (II) complexes are more stable, but the Zinc (II) complexes are more suitable due to their good stability combined with great photophysical properties. We also report the polymerization of 4'-ethynyl-2, 2': 6', 2''-terpyridine as substance, which combines in the structure the possibility to make common covalent and non-covalent polymers. Last part of this thesis considers the synthesis of phosphole-based substances, which make as well as the terpyridine derivatives full conjugated system. Keywords: terpyridine, complexation, stability constant
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Nové inhibitory HIV proteasy: návrh, synthesa a testování aktivity
Schimer, Jiří ; Konvalinka, Jan (advisor) ; Obšil, Tomáš (referee)
More than 20 years after its discovery HIV protease still remains one of the primary targets in HIV treatment. Currently there are 9 approved protease inhibitors on the market. However, due to immense replication rate and the high error prone nature of reverse transcriptase, resistance to each of them has already been described. Therefore, the search for new protease inhibitors with different binding mode is still active. A novel type of protease inhibitors (1, 4-benzodiazepine analogs) was recently discovered in our laboratory. Even though this new class of inhibitors is highly potent (Ki' in range of 10-9 ), it also has several undesirable qualities, such as low solubility and a high number of stereogenic centers. Primary objective of this study was to try to prepare more soluble compounds with lower number of possible stereoisomers, enzymologically characterize its binding to the wild-type and mutated HIV protease and to determine its structure in the complex with the enzyme. A small library of 1, 4-benzodiazepine inhibitors of HIV protease was synthesized and fully characterized using NMR spectroscopy and mass spectroscopy. The number of stereogenic centers was successfully reduced from 4 to 2 without loosing activity of the inhibitor. The improvement in solubility was always associated with a...
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název v anglickém jazyce není uveden
Pospíšilová, Eva ; Paleček, Jiří (advisor) ; Kršiak, Miloslav (referee) ; Rokyta, Richard (referee)
Tissue injury leads to increased sensitivity to noxious and innocuous stimuli due to mechanisms of peripheral sensitisation of primary nociceptors and central sensitization of neurons in the spinal dorsal horns. The subpopulation of capsaicin - sensitive sensory neurons plays an important role in this process. The capsaicin - sensitive neurons express capsaicin TRPV1 receptors (transient receptor potential 1) on their peripheral and central terminals, local high concentration capsaicin treatment can induce regional destruction of these endings. It is well estabilished that TRPV1 receptors play the key role in neural transmission of nociceptive information and its modulation. The aims of this study were to investigate the role of capsaicin - sensitive primary afferent fibers and the involvement of peripheral and central TRPV1 receptors in the development of hypersensitivity after surgical tissue trauma, to test the effect of high concentration capsaicin and the specific TRPV1 antagonist treatment on postoperative pain and to enlighten the function of central TRPV1 receptors in the neural mechanisms of nociception. Using behavioral testing methods, the responses to mechanical (Von Frey filaments) and thermal stimuli (radiant heat source) were tested on the rat plantar incision model of surgical pain...
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Formation of national identity in a multinational environment: Paris immigrants in the years 1848-1900
Olšáková, Doubravka ; Vlnas, Vít (advisor) ; Šedivý, Ivan (referee) ; Galmiche, Xavier (referee)
The thesis deals with the problem of formation national identity in a multinational milieu on the case study of immigrants in Paris 1848-1900. This study is based on the analysis of archival books stored in Archives de Paris. The theories of nationalism are confronted with the quantitative analysis of data mentioned in the application forms. The analysis is made for Germany, Luxembourg, Bohemia and Hungary. The general trend tends toward the identification with State-Nation, the only exception is Bohemia. The majority of immigrants from this country professed to Austria. However, the general trend pointed out that the delay of mass anticipation was bigger than supposed by the theoretical issues. This phenomenon is due to the weak social mobilization caused by the limited capabilities and possibilities of leading local elites. The author tries to explain the Czech exception through the semiotic analysis of collective memory transformation made on the examples of notions frontier and out/and. Powered by TCPDF (www.tcpdf.org)
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Study and comparison of main kinds of evolutionary algorithms
Štefan, Martin ; Holeňa, Martin (advisor) ; Gemrot, Jakub (referee)
Evolutionary algorithms belongs among the youngest and the most progressive methods of solving difficult optimization tasks. They received huge popularity mainly due to good experimental results in optimization, a simplicity of the implementation and a high modularity, which is an ability to be modified for different problems. Among the most frequently used Evolutionary algorithms belongs Genetic Algorithm, Differential Evolution and Evolutionary Strategy. It is able to apply these algorithms and theirs variants to both continuous, discrete and mixed optimization tasks. A subject of this theses is to compare three main types of algorithms on the catalyst optimization task with mixed variables, linear constraints and experimentally evaluated fitness function.
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Language analysis of the early printed book Life of the blessed Agnes... from 1666
Turková, Táňa ; Adam, Robert (referee) ; Kučera, Karel (advisor)
This thesis gives a basic language characteristic of the ear1y printed book Life ol the Blessed Agnes... from 1666 from the orthographical, phonetic, morphological, syntactic and lexical perspective. Transcription of the text of this record is also part of the thesis. The examined text is a translation from Latin which originated at the beginnig of the 15th century and was printed according to an old manuscript in 1666. The printing contains extra explanatory marginalia which were added by the publisher. The legend was printed using the Moravian orthography and contains some mistakes due to trascription of the digraphic orthography which was used in the old manuscript. The quantity of vowels is marked, however the graphic form of the printing gives information more about the quantity of Czech in the 1 i h century rather than of Czech in the 15th century. The graphics of the legend reflects some changes which were happening in the phonetic system at that time but the phonetic Czech of the legend basically agrees with the Czech today. More differences in comparison with present Czech can be found in morphology. Compared to today' s Czech concrete formative differences which originated in Old Czech (system oftenses, participle forms, dec1ination of some nouns and numerals) show themselves within particular...
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Expression of cholinergic gene locus in a mouse model of Alzheimer's disease
Zimčík, Pavel ; Doležal, Vladimír (advisor) ; Teisinger, Jan (referee)
(anglický jazyk) The most common senile dementia, Alzheimer disease (AD), is characterized by a decline of memory and high cognitive functions. Typical post-mortem brain lesions are extracellular amyloid deposits, intracellular neurofibrilary tangles and ruined cholinergic and other neurotransmitters systems. Connection between damaged central cholinergic system and beta-amyloid accumulation remains obscure. We examined parietal cortex of young adult (7- month-old) female APPswe/PS1dE9 double transgenic mice which develope beta-amyloid fragments at high rate. Cholinergic synapses of these mice demonstrate functional presynaptic (stimulated acetylcholine release) as well as postsynaptic (muscarinic receptor-induced G- protein activation) deficits and reduction of cholinergic markers. The mRNA levels of choline acetyltransferase, vesicular acetylcholine transporter and M1 to M4 subtypes of muscarinic receptors were determined in transgenic and littermate controls using qPCR. Obtained experimental data does not show any changes in measured mRNA levels. These observations indicate that reduction of cholinergic synaptic markers and function is due to posttranscriptional events.
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Chemistry education at secondary schools of civil engineering in the Czech Republic
Dvořák, Martin ; Čtrnáctová, Hana (advisor) ; Kolář, Karel (referee) ; Rovnaník, Pavel (referee)
Title Chemistry education at secondary schools of civil engineering in the Czech Republic Abstract The goal of this work is to evaluate the chemistry education at secondary schools of civil engineering in the Czech Republic, which provide education of four-year study programs with school leaving exam. At first, question form of data gathering was used at the part of these schools. The general goal was narrowed by analyzing the answers of a questionnaire and the next work was concentrated on creating a study material containing themes of the chemistry of building materials. This material was used during the period of its creation and was modified due to the reactions of the students. The material was then extended with themes of general, inorganic, organic chemistry and biochemistry. The learning material was extended to the form of practice book, which has been used as a main educational tool for the chemistry education. The learning material was evaluated by theoretical methodology and by anonymous questionnaire filled by students. The objective evaluation of the impact of the learning material on the school grades was analyzed through five years. Key words Chemistry of building materials, secondary schools, learning material, workbook.
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Self-harm prevention in inpatients
Necid, Petr ; Marx, David (advisor)
The aim of this diploma work is to explore tactics which would help serve as a preventive measure from inpatients inflicting self-harm. This work was conducted in selected psychiatric departments throughout the Czech Republic by using an anonymous questionnaire investigation. Only fifty percent of the departments have internal guidelines for detection of at risk patients. Eighty-eight percent of departments have an internal system for reporting extraordinary events. Many of these departments have advanced technical equipment, but there are still some departments with technical equipment at lower levels, probably due to the high costs associated. Only two departments are using scales for evaluation of admitting patients. Fifty percent of the departments evaluate risks of self-harm for admitting patients. Self-harm was present in all departments in this study; seventeen percent of departments did not report any number of suicide attempts and forty two percent of the departments did not report any number of the self-harm attempts. The results are showing a positive trend in the role of prevention, as well as increasing the safety level within individual departments. The data are also showing that not all of departments are taking sufficient measures to ensure prevention. Clear evidence of self-harm and suicide...
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Synthesis of bisquaternary nonsymmetric acetylcholinesterase reactivators
Sopr, Stanislav ; Kopecký, Kamil (referee) ; Doležal, Martin (advisor)
Stanislav Sopr: PREPARATION OF BISQUARTERNARY NON-SYMETRIC ACETYLCHOLINESTERASE REACTIVATORS Abstract The acetylcholinesterase (AChE) reactivators cause the re-activation of AChE activity after inhibition by organophosphorus compounds (OP). Such OP inhibitors were formerly developed as pesticides, but they were further used as chemical warfare agents due to their extremely high inhibition of cholinesterases. In this diploma thesis, 18 novel AChE reactivators were prepared. Their ability to reactivate paraoxon-inhibited AChE was evaluated in vitro via Ellman's method and compared to 3 standard commercial compounds (pralidoxime, obidoxime and HI-6). Any newly prepared compound was superior to known standards at 10-4 mol/l concentration. However, three novel compounds were able to exceed reactivation ability of known standards at 10-6 mol/l concentration and one novel compound exceeded reactivation limit for further potential in vivo evaluation.
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