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Roof structure of terminal building
Matouš, Petr ; Bukovská, Pavla (referee) ; Röder, Václav (advisor)
The supporting structure of the roof of terminal building is designed as a combination of trusses glued laminated timber, purlins and columns of solid wood and steel poles supports and rods. Truss is mounted on steel columns and supported by steel lattice structures and wooden pillars.
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Ecoduct on Motorway D1
Matouš, Petr ; Boštík, Jiří (referee) ; Glisníková, Věra (advisor)
The master’s thesis focuses on suitable design of an ecoduct on the highway D1 near Jihlava. It includes a structural analysis of reinforced concrete strip footings and wooden beams in all phases of construction. The material of the main bearing system is glued laminated timber GL24h. An important part of three-jointed ecoduct wooden arched beams is well-chosen isolation.
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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.
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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...
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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...
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Synthesis and Reactivity of Enynes with Terminal Double Bond
Grobař, Bartoloměj ; Matouš, Petr (advisor) ; Opálka, Lukáš (referee)
Charles University in Prague Faculty of Pharmacy in Hradec Králové Department of organic and bioorganic chemistry Candidate: Bartoloměj Grobař Supervisor: PharmDr. Petr Matouš, Ph.D. Title of thesis: Synthesis and reactivity of enyns with terminal double bond This work focuses on synthesis of structures containing terminal vinyl moiety and their subsequent reactivity. We tested various approaches that lead to formation of enynes, which are then cyclized using gold complex catalyst into tetrahydropyridines. Both utilize the addition of propargylamine protected by 4-methoxybenzenesulfonyl group to substituted butynone and methoxyphenyl propiolates. Tetrahydropyridine molecules that are successfully created, are further derivatized forming polycyclic structures.
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Synthesis of Ortho-Condensed Nitrogen Heterocycles Using Gold Complexes
Makaj, Petr ; Matouš, Petr (advisor) ; Kuneš, Jiří (referee)
5 ABSTRACT Charles University, Faculty of Pharmacy in Hradci Králové Department of Organic and Bioorganic Chemistry Candidate: Petr Makaj Supervisor: PharmDr. Petr Matouš, Ph.D Title of Thesis: Synthesis of Ortho-Condensed Nitrogen Heterocycles Using Gold Complexes This diploma thesis is focused on the preparation of pyridopyridine derivatives using gold-catalyzed cyclizations. The synthesis is based on MBS-protected propargylamine, which after substitution with aryl using Sonogashira coupling reacts with tert-butyl (3- oxopent-4-ynyl)carbamate to form substituted 1,5-enyne. The enyne thus prepared then undergoes cycloisomerization using tris(2- furanyl)phosphinegold(I)chloride as a catalyst to form pyridopyridine. Substances with this scaffold can be further used to synthesize potentially biologically active structures. Keywords: gold catalysis, cyclization, pyridopyridine derivatives, 1,8-naphthyridine derivatives
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Synthesis of Chromenopyridines with the New All-Carbon Quaternary Centre
Sedláček, Patrik ; Matouš, Petr (advisor) ; Krátký, Martin (referee)
Charles University in Prague Faculty of Pharmacy in Hradec Králové Candidate: Patrik Sedláček Supervisor: PharmDr. Petr Matouš, Ph.D. Title of thesis: Synthesis of Chromeno[3,4-c]pyridines with New All-Carbon Quaternary Centre This diploma thesis focuses on the synthesis of 3,4-disubstituted pyridine derivatives and their subsequent cyclization to form chromeno[3,4-c]pyridine derivatives with a new all-carbon quaternary center. Phenyl-propiolate reacts with an aryl-substituted propargyl amine protected with 4- methoxybenzenesulfonyl group to form a 1,5-enyne. Substituted 1,5-enyne undergoes intramolecular cyclization catalyzed by tri(2-furyl)phosphinogold(I)chloride [AuCl(TFP)] to form the corresponding dihydropyridine. In the presenece of concentrated H2SO4, dihydropyridine undergoes carbocyclization forming the corresponding chromenopyridine with a new all-carbon quaternary center. The compounds prepared and their derivatives could find application as potentially biologically active substances and intermediates in organic synthesis.
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Synthesis of ceramides derived from 6-hydroxysphingosine
Kavuljak, Juraj ; Opálka, Lukáš (advisor) ; Matouš, Petr (referee)
Title of the Master thesis: Synthesis of ceramides derived from 6-hydroxysphingosine Candidate: Juraj Kavuljak Supervisor: PharmDr. Lukáš Opálka, Ph.D. Consultant: Mgr. Veronika Ondrejčeková Charles University, Faculty of Pharmacy in Hradec Králové Skin Barrier Research Group, Department of Organic and Bioorganic Chemistry Ceramides (Cer), belong to the group of sphingolipids naturally found in each cell. One of their principal functions is cell signaling. We can find Cer in the uppermost layer of epidermis (stratum corneum), where the concentrations of these lipids are highest in the whole human body. Cer form an intercellular multi-lamellar lipid matrix. This lipid mass is composed of cholesterol and free fatty acids as well. The major function of stratum corneum is to protect the body from the excesive transepidermal water loss, provide internal homeostasis and create a protective barrier against harmful substances from external environment. Cer are amides of long aminoalcohols with a fatty acid attached to their primary amino group. 6-hydroxysphingosine (H) is specific for human epidermis, but its function and biosynthesis in skin is still not completly understood. Some studies showed lower concentrations of 6-hydroxysphingosine-based Cer in skin of patients suffering from atopic dermatitis....
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Synthesis and evaluation of potential antimicrobial agents
Sýkorová, Jana ; Krátký, Martin (advisor) ; Matouš, Petr (referee)
Antibiotic resistance is a global problem and the development of new drugs, among other approaches, should contribute to mitigating the consequences. All newly prepared compounds are based on the 4,6-dimethylpyrimidine-2-amine, in some syntheses its derivative sulfamethazine was used as a starting compound. The starting molecule was chosen based on the antimicrobial activity of 4,6-dimethylpyrimidine-2-amine derivatives. The aim of three one-step syntheses was to prepare sulfonamides from 4,6-dimethylpyrimidine-2-amine and corresponding sulfonyl chlorides. Other ten also one-step reactions led to the preparation of Schiff bases, which are mostly based on salicylaldehyde and benzaldehyde derivatives. Different methods were used, yields ranged from 13 % to 48 % for sulfonamides and from 13 % to 96 % for Schiff bases. All thirteen compounds were tested for antibacterial (against selected G+ and G- strains) and antifungal activity using the microdilution broth method. In general, the compounds were ineffective against G- bacteria and, on the other hand, showed the greatest activity (i.e., lowest minimum inhibitory concentrations, MIC) against fungi. Sulfonamides were ineffective. The lowest MICs for both fungi (3.9 µmol l-1) and bacteria (15.62 µmol l-1) were found for...
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