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Preparation of organocatalysts derived from thiourea containing saccharide units
Řehůřková, Tereza ; Veselý, Jan (advisor) ; Smrček, Stanislav (referee)
4 ABSTRACT This diploma thesis is focused on the synthesis of new bifunctional thiourea organic catalysts containing a carbohydrate moiety, in particular D-glucose with modification on the primary hydroxyl group. The first part of this diploma thesis describes a modification of synthesis of the known bifunctional thiourea catalyst with 2,3,4,6-tetra-O-acetyl-β-D-glucopyranose and (1R,2R)-diaminocyclohexane. The second part is dedicated to the synthesis of new bifunctional thiourea catalysts with modification of the carbohydrate moiety. We focused on per-O-acetyl-β-D-glucopyranose derivatives with pefluoroalkyl moiety on the primary hydroxyl group. We examined different ways of the preparation of 6-O-perfluoroalkylated glucose derivatives. These perfluoroalkylated carbohydrate compounds were transformed into corresponding glycosyl isothiocyanates. Those derivatives upon treatment of (1R,2R)-diaminocyklohexane or 3,5- bis(trifluormethyl)aniline afforded new bifunctional thiourea organocatalysts.
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Index ekonomické svobody, případ České republiky
Shrbený, Filip ; Stroukal, Dominik (advisor) ; Máslo, Lukáš (referee)
We have identified number of possible advices for the Czech Republic to improve its rating for both Heritage Foundation and Fraser Institute Economic Freedom Index, which often leads to top 10 countries in the world. These advices range from cuts in government spending, betterment in judicial system, to the establishing healthier environment for startups and advices to combat corruption. We further noticed some divergence between above mentioned indexes and managed to evaluate those indexes, which showed the simplicity yet usefulness of Heritage EFI and flexibility and sensitivity of the Fraser EFI. Weak sides of the research were noted and ideas for further research were given.
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Heterocyclic Compounds with Antimycobacterial Activity
Herzigová, Petra ; Klimešová, Věra (advisor) ; Potáček, Milan (referee) ; Pytela, Oldřich (referee)
The dissertation thesis belongs to the conception of the research of potential antimycobacterial compounds. The aim of this work is synthesis of sulphide pyridine derivatives and the relationship between structure and antimycobacterial activity. Within the framework of this Thesis, the 112 substituted derivates of 4-(subst. fenylalkylsulfanyl)pyridine-2-carboxylic acid were synthesized. Antimycobacterial activity of prepared substances has been tested under in vitro conditions against M. tuberculosis, and non-tuberculous mycobacteria M. avium and M. kansasii. The series of 4-(subst. phenethylsulfanyl)pyridine-2-carbothioamide (MIC 1-32 µmol/L) represents the most active substances (MIC 1-32 µmol/L). These derivates don't reach the activity used antituberculosis drugs against M. tuberculosis, but their activities against M. avium exceed that of isoniazid. The synthesis of new structures as potential antimycobacterial compounds forms the second part of Thesis. All synthesis is based on the use of bis- arylimidoyl chlorides of oxalic acid of as starting material. None of prepared new compounds don't display an interesting antimycobacterial activity.
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Synthesis of carboxyxanthone derivatives as building blocks for enantiomeric pure compounds. Synthesis and structure elucidation of xanthone derivative (XD) 2-carboxy-6-methoxyxanthone (XD-2)
Heczková, Jana ; Opletalová, Veronika (advisor) ; Zimčík, Petr (referee)
Charles University in Prague, Faculty of Pharmacy in Hradec Králové Department of Pharmaceutical Chemistry and Drug Control Candidate Jana Heczková Consultant Professora Doutora Madalena Maria de Magalhães Pinto, Assoc. Prof. RNDr. Veronika Opletalová, Ph.D. Title of Thesis Synthesis of carboxyxanthone derivatives as building blocks for enantiomeric pure compounds. Synthesis and structure elucidation of xanthone derivative (XD) 2-carboxy-6-methoxyxanthone (XD-2) The importance of xanthone derivatives is considerable. They possess large variety of biological and pharmacological activities. Many of them proved to be important building blocks for synthesis of new compounds. Chirality is a fundamental property of biological systems and reflects the underlying asymmetry of matter. Almost one-third of all drug sales worldwide are chiral compounds and the authorities recommend that the chiral drugs should be saled in pure enantiomeric forms because enantiomers may differ both quantitatively and qualitatively in their biological activities. At one extreme, one enantiomer may be devoid of any biological activity; at the other extreme, both enantiomers may have qualitatively different biological activities. Enantiomers also differ in bioavailability - one enantiomer can be more bioavailable than the other,...
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DEVELOPMENT OF AN ORGANIZATIONAL BEHAVIOUR IN CAUSED BY ICT
Tichý, Ondřej ; Hynek, Josef (referee) ; Mikoláš, Zdeněk (referee) ; Půža, Bedřich (referee) ; Němeček, Petr (advisor)
The thesis covers a research into the relationship between the Czech organizations and employees and modern information and communication technologies (abbreviated as ICT). From the perspective of organizations, the research focuses on the specific technologies that have been implemented in recent years. How have the technologies been proved and whether they managed to influence an organizational structure of companies. The research is also interested in the impact of these technologies on employees, especially on their productivity. The research, carried out between foreign articles, showed that in countries such as China or USA people suffered from a technostress. The technostess could be described as a stress induced by these technologies. Then, the technostress has a negative impact to the mentioned labor productivity. The introductory part of the text contains secondary research, which focuses on two basic topics. The first part concerns the description of an organization. It indicates what that organization is, and yet the historical opinions on the organizations are also described here. Furthermore, there is described the term like an organizational behavior and its integration into the functioning of the organization. Followed by a section, which defines the position of the individual within the organization. The next section contains a description of the organizational structures. The second basic topic within the secondary research describes ICT. But there is not described a technical specification, there is a description of their importance to the organization, including the relationship of employees of organizations to these technologies. The second half of this dissertation thesis contains two primary researches that are built on the previous theoretical part. Its objectives are: 1) the creation of a model which would includes ICT and also shows the ICT’s impact on a company; 2) to develop a methodology for determining the benefits of ICT to the company and to set them on the basis of the results of the research carried out in this thesis; 3) to identify the latest trends in the implementation of ICT in organizations in the ICT sector in the Czech Republic; 4) to determine whether the current organizational structures of the examined companies are affected by ICT; 5) to ascertain whether the modern ICT affect Czech employees in a negative way, so that caused their lower productivity; and 6) make some recommendations regarding the implementation of ICT for other companies in the Czech Republic. The result of the thesis is the synthesis of knowledge acquired on the basis of the analytical part. During the data collection the inductive and deductive methods were used and the both studies yielded the following conclusions. The employees who use these technologies, do not mostly suffer from the technostress, despite the fact that there was proved a weak dependence between the technostress and a lower labor productivity by the statistical test. The research into the organization also showed that larger Czech companies from the ICT sector tend to focus on the short-term benefits within acquisition of the new ICT. The examined link between the ICT and organizational structures of companies was not demonstrated. The further evaluation showed that the companies mostly acquired software, which was specially developed for them. Finally, it can be considered as a trend in the acquisition of the new ICT to the Czech organizations.
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Design and synthesis of selective gallium(III) chelators
Krchová, Tereza ; Lorenc, Miroslav (referee) ; Kotek, Jan (advisor)
This bachelor thesis is focused on the preparation of two new ligands (based on the 1-oxa-4,7-diazacyclononane skeleton), which would be potentially suitable for fast and selective complexation of Ga(III). Complexes of these ligands could find applications in radiodiagnostics (PET, SPECT), or as a new class of contrast agents for MRI based on proton chemical exchange saturation transfer (CEST). This thesis also describes the preparation of 1-oxa-4,7-diazacyclononane and attempts of preparation of N-benzyloxycarbonylaziridine. Thesis also includes a description of radiodiagnostic and radiotherapeutic methods of nuclear medicine. It also discusses the method of magnetic resonance tomography (MRI), especially the method using CEST contrast agents. Thesis contains an overview of the use of Ga(III) radioisotopes in radiomedicine.
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Relationship between Structure and Biological Activity of new Modulators of Acetylcholinesterase
Komlóová, Markéta ; Doležal, Martin (advisor) ; Kuneš, Jiří (referee) ; Jampílek, Josef (referee)
Charles University in Prague, Faculty of Pharmacy in Hradec Králové Department: Dpt. of Pharmaceutical Chemistry and Drug Control Student: Mgr. Markéta Komlóová Supervisor: prof. PharmDr. Martin Doležal, Ph.D. Title of Doctoral Thesis: Relationship between structure and biological activity of new modulators of acetylcholinesterase This work focuses on the preparation of peripherally acting AChE inhibitors as a potential treatment of myasthenia gravis. These compounds could also be used as a pre- treatment of poisoning by organophosphorus AChE inhibitors. They can occupy the active site of an enzyme making it inaccessible for irreversible inhibitors. Compounds used in this indication should fulfill these requirements: inhibit efficiently AChE (standards currently used in the treatment were chosen for the comparison of the inhibitory efficacy), have selective effect on AChE and not to cross the blood-brain barrier in order to lower the possible side effects. Six series of bisquaternary compounds were prepared. Their inhibitory ability was determined in vitro against human erythrocyte or recombinant AChE and human plasmatic BChE. According to inhibitory ability values acquired, a structure - activity relationships were investigated in every series. A few compounds with significant affinity towards...
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