National Repository of Grey Literature 177 records found  1 - 10nextend  jump to record: Search took 0.01 seconds. 
Xanthone-boronic acids: An insight into the synthesis of borylated xanthone derivates
Houngbedji, Priam-Amedeo ; Doležal, Martin (advisor) ; Zitko, Jan (referee)
CHARLES UNIVERSITY FACULTY OF PHARMACY IN HRADEC KRÁLOVÉ DEPARTMENT OF PHARMACEUTICAL CHEMISTRY AND PHARMACEUTICAL ANALYSIS DIPLOMA THESIS XANTHONE-BORONIC ACIDS: AN INSIGHT INTO THE SYNTHESIS OF BORYLATED XANTHONE DERIVATIVES Supervisor: prof. PharmDr. Martin Doležal, Ph.D. HRADEC KRÁLOVÉ 2021 PRIAM-AMEDEO HOUNGBEDJI Abstract - English The development of Bortezomib 5 and discovery of its potential in the treatment of multiple myeloma has sparked hope, and a close attention is paid in medicinal chemistry to the synthesis of boronic acid derivatives as well as the evaluation of their anticancer, antimicrobial, and other activities. Parallelly, xanthones and xanthone derivatives are compounds thoroughly studied for their potential in the treatment of cancer, and their good antimicrobial, anti-inflammatory, antiviral and anticonvulsant activity. It is only natural that efforts are oriented towards the synthesis of xanthone boronic derivatives. 3,6-Dihydroxyxanthone 10 was chosen as a precursor for the development of a procedure to borylate xanthones, mainly due to its easy synthesis and availability. From 10, 3,6-ditrifylxanthone 11 was easily prepared. The synthesis of 3,6- bis(pinacolatoboron)xanthone 8 from 11 was achieved using bis(pinacolatodiboron) B2pin2 as a borylation agent under Pd(dppf)Cl2 catalysis...
Synthesis of Alkaloid-like Compounds with Quaternary Carbon Centers
Jansa, Petr ; Matoušová, Eliška (advisor) ; Baszczyňski, Ondřej (referee) ; Nováková, Veronika (referee)
Synthesis inspired by natural products has a long tradition in drug development. Because the structure of bioactive natural compounds is often very complex, preparation of their derivatives requires the development of specific synthetic procedures. This thesis focuses on derivatives of certain alkaloids from the Amaryllidaceae plant family as examples of such compounds. The thesis explores the possibilities of preparing polycyclic compounds that contain the structural motif present in tazettine, crinine, or mesembrine-type alkaloids. This motif includes a quaternary all-carbon center, for which a method involving a tandem cyclization/Suzuki coupling reaction and a halocarbocyclization was developed and optimized in this work. The scope of these reactions was studied, and variously substituted products containing oxygen and nitrogen cycles were prepared. Furthermore, methods for the synthesis of N-alkylated derivatives, dehydrohalogenation to form a double bond, or various mainly oxidative modifications of the cycle adjacent to the aromatic ring were developed. After developing a method for the preparation of enantiomerically enriched starting material, an asymmetric version of the entire synthesis was successfully performed. Finally, biological properties of selected compounds were studied. Some...
Complete series of lanthanide oxalates: Structure and properties
Uríková, Daniela Veronika ; Tyrpekl, Václav (advisor) ; Hynek, Jan (referee)
Metal oxalates are salts of very low solubility allowing an easy precipitation of metal ions from the acidic aqueous solutions into crystalline material. Due to this property, oxalates have an important role in the technology of lanthanides and actinides. It is namely the separation of actinides from the spent nuclear fuel that is its industrial application of interest. 4f-lanthanides are often used as 5f-actinides surrogates when optimizing or modelling the precipitation process. A synthetic route for homogeneous precipitation of oxalates based on the thermal decomposition of oxamic acid was developed by our research team. The present work deals with further investigation into the structure and morphology of simple lanthanide oxalates. The synthesis products, developed microcrystals, were studied by means of solid-state analysis (optical microscopy, single crystal X-ray diffraction, X-ray powder diffraction, TGA, SEM, AFM). Among the known, the previously not-specified structures of Er2(C2O4)3∙6H2O and Yb2(C2O4)3∙6H2O were obtained and refined. According to our observations, the synthesized oxalates form two isostructural series: decahydrates and hexahydrates. Structurally, both types of Ln oxalates form 2D frameworks that are stacked together in one direction and connected by hydrogen bonds to...
The development of reliable method for glucosylation and lactosylation of sphingolipids
Hošek, Adam ; Opálka, Lukáš (advisor) ; Karabanovich, Galina (referee)
Title of the master thesis: The development of reliable method for glucosylation and lactosylation of sphingolipids Candidate: Adam Hošek Supervisor: PharmDr. Lukáš Opálka, Ph.D. Consultant: Dr. Georgios Paraskevopoulos, Ph.D. Charles University, Faculty of Pharmacy in Hradec Králové Skin Barrier Research Group, Department of Organic and Bioorganic Chemistry Ceramides are hydrophobic sphingolipids consisting of a sphingoid base and an acyl chain. They are found in the stratum corneum, the uppermost layer of the epidermis, where they are important part of the skin barrier, but they can also be found in brain tissue and inside human cells. Glucosylceramides are the simplest glycosphingolipids, and they contain a single glucose molecule in their structure. They are found in all types of human cells, where they not only serve as precursors for the biosynthesis of other, more complex glycosphingolipids, but also have their own physiological functions. The most significant is their influence on cell growth, development, differentiation and apoptosis. Disruptions in their synthesis or degradation can lead to serious health problems and are also a risk factor for the future development of a wide range of diseases. Their total absence in the body is incompatible with life. A more thorough study of their...
New fungal fucosidases and their synthetic potential
Glozlová, Michaela ; Beránek, Martin (advisor) ; Matoušková, Petra (referee)
Charles University Faculty of Pharmacy in Hradec Králové Department of Biochemical Sciences Candidate: Bc. Michaela Glozlová Supervisor: prof. PharmDr. Martin Beránek, Ph.D. Consultants: doc. RNDr. Pavla Bojarová, Ph.D., Mgr. Pavlína Nekvasilová Title of diploma thesis: New fungal fucosidases and their synthetic potential The literary research focuses on α-L-fucosidases, their occurrence, functions, and use in the synthesis of fucosylated compounds, which were also a part of the research, particularly their presence in the human body and involvement in pathological conditions. Furthermore, it explores the oligosaccharides found in human milk, their impact on infant health, and their synthesis, which can be facilitated through the use of α-L-fucosidases. The experimental section involves the analysis of a library of filamentous fungi with the aim of identifying a representative strain with α-L-fucosidase activity towards pNP-α-L-fucoside. Recombinant α-L-fucosidases were selected based on searches in genetic databases and prepared. The feasibility of their production in Pichia pastoris and Escherichia coli was tested, and the produced enzymes were purified by ion exchange chromatography, characterized and their regioselectivity and synthetic potential for the synthesis of fucosylated...
Synthesis and reactivity of selected [3]dendralene derivatives
Štemberová, Marie ; Pour, Milan (advisor) ; Matouš, Petr (referee)
Charles University in Prague Faculty of Pharmacy in Hradec Králové Department of Organic and Bioorganic Chemistry Candidate: Marie Štemberová Supervisor: prof. RNDr. Milan Pour, Ph.D. Supervisor - specialist: PharmDr. Zbyněk Brůža, Ph.D. Title of Diploma Thesis: Synthesis and reactivity of chosen derivates of [3]dendralenes This diploma thesis is focused on the preparation of derivates of [3]dendralenes containing electron-withdrawing ester groups. The synthesis is based on a palladium- catalyzed Migita-Stille coupling between stannylated esters and iodinated acrylate which are prepared from methyl-propiolates. Subsequently these dendralenes undergo Dien-transmissive Diels-Alder reaction with electron-deficient dienophile N-phenylmaleimide, resulting in formation of polycyclic structures.
Synthesis of novel inhibitors of human topoisomerase based on highly substituted phenyl scaffold
Domanský, Miroslav ; Zitko, Jan (advisor) ; Zimčík, Petr (referee)
Charles University in Prague, Faculty of Pharmacy in Hradec Králové Supervisor: Assoc. Prof. PharmD. Jan Zitko, PhD. Consultant: Mgr. Marek Kerda Author: Miroslav Domanský Title of diploma thesis: Synthesis of novel inhibitors of human Topoisomerase based on highly substituted phenyl scaffold. Despite progress in anticancer therapy, cancer is still one of the leading causes of death in the world. Patients treated with current anticancer therapy suffer from many side effects. This is caused by the low selectivity of the current drugs. The development of chemotherapeutics aims to prepare more selective and therefore better tolerated anticancer drugs. Topoisomerases are nuclear enzymes occurring in every cell. They have an essential role - to preserve DNA and repair it. Topoisomerase isoform IIα is an isoform that controls and edits the conformation of DNA during cell replication. Its expression is highly elevated in proliferating cells. That makes it a good target for anticancer drugs. The design of synthesized molecules is based on previously reported ATP-competitive inhibitors of human topoisomerase IIα. Alterations of 3,4-dichloro-5-methyl-N-phenyl-1H- pyrrole-2-carboxamide have been synthesized based on Computational-Aided Drug Design. The in silico study is based on the previous discovery of the...
Synthesis and evaluation of potential biologically active rhodanine derivatives and analogues
Šimková, Adéla ; Krátký, Martin (advisor) ; Matouš, Petr (referee)
The topic of this thesis is the synthesis of rhodanine derivatives and evaluation of their biological activity, particularly as potential cholinesterases inhibitors. This group of compounds is important for treatment of many diseases, e.g., Alzheimer's disease or myasthenia gravis. All synthetized compounds are based on structure of rhodanine (2-thioxothiazolidine- 4-one), which is an important heterocyclic compound with a wide spectrum of biological properties. Its structure can be modified in many ways, which can be used in the development of new drugs. Its derivatives have been shown to have, for example, anti-inflammatory, anticancer, antibacterial and antifungal activities, as well as inhibitory activity against several enzymes, e.g., cholinesterases. Seventeen compounds were synthesized in sufficient amount for characterisation and assessment of biological activity (7-93 %). Most of them are amides based on the structure of 2-thioxothiazolidine-4-one and thiazolidine-2,4-dione, that were prepared by carbodiimide- mediated coupling, other derivatives are based on the structure of 2-thioxothiazolidine-4-one and from 2,4-dioxothiazolidine-3-acetic acid. These compounds were prepared by Knoevenagel condensation in glacial acetic acid. All compounds were tested for their inhibitory activity...
Synthesis and evaluation of potential antimicrobial drugs
Pflégr, Václav ; Krátký, Martin (advisor) ; Doležal, Martin (referee) ; Brulíková, Lucie (referee)
Charles University, Faculty of Pharmacy in Hradec Králové Training Workplace Department of Organic and Bioorganic Chemistry Doctoral Degree Program Bioorganic Chemistry Candidate: Mgr. Václav Pflégr Supervisor: doc. PharmDr. Mgr. Martin Krátký, Ph.D. Title of Doctoral Thesis: Synthesis and evaluation of potential antimicrobial drugs The dissertation thesis reports some results achieved within the framework of a doctoral project dealing with the synthesis and evaluation of potential antimicrobial drugs. The main goal was to obtain new derivatives of isoniazid and its analogues acting against Mycobacterium tuberculosis and non-tuberculous mycobacteria, optimally including resistant strains. A partial aim was the preparation of peptide carriers for antituberculosis drugs, which, in addition to the development of new molecules, is another promising direction for the development of new therapeutic strategies against tuberculosis. The theoretical part of the dissertation overviews the issue of tuberculosis. The aetiology of the disease, the morphology of the cell wall of mycobacteria and selected epidemiological data are presented there. The treatment and characteristics of clinically used drugs are described in detail, this chapter is followed by a brief research review of promising clinically evaluated...
Synthetic bodies
Veselá, Lenka ; Kolářová,, Kateřina (referee) ; Klodová, Lenka (referee) ; Fajnor, Richard (advisor)
In my dissertation thesis grounded in the notion of synthetic bodies, I reflect on the fact that we are not enclosed entities, but lively structures formed in relation to the environments which surround and entangle us. With a focus on industrially manufactured chemicals, which have become ubiquitous on Earth in the Anthropocene, I examine the far-reaching effects of what it means to be a synthetic body in a world permeated and transformed by man-made technologies. Through the collective publication and exhibition project Synthetic Becoming and individually developed intervention which localizes the effects of anthropogenic chemical pollution on our sadness, irritability, anxieties, inability to concentrate, and feelings of despair and hopelessness, I explore how we can live well in the context of changes caused by industrial modernity. How can we come to terms with our open and permeable, and thus also vulnerable and wounded bodies? How can we understand who we are becoming with anthropogenic chemicals? How can we accept and affirm the part of ourselves which is co-constituted through industrial production, distribution, and consumption? How can we resist, survive, and keep going — with and despite industrial chemicals?

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