National Repository of Grey Literature 24 records found  1 - 10nextend  jump to record: Search took 0.02 seconds. 
Synthesis of novel quinazoline derivatives as a potential multipotent therapeutics against Alzheimer's disease
Tošnerová, Daniela ; Karabanovich, Galina (advisor) ; Matouš, Petr (referee)
1 ABSTRACT Charles University, Faculty of Pharmacy in Hradec Králové Department of: Organic and Bioorganic Chemistry Mentor: Ing. Galina Karabanovich, Ph.D. Consultant: Ing. Barbora Svobodová, Ph.D. Student: Daniela Tošnerová Title of Thesis: Synthesis of novel quinazoline derivatives as a potential multipotent therapeutics against Alzheimer's disease Alzheimer's disease (AD) is a severe neurologic disorder. Current treatments only temporarily delay the progression of disease. The main limiting factor for developing of new therapeutic compounds is the simultaneous presence of multiple pathologies. Thus, a new group of potential drugs called multi-target directed ligands (MTDLs) emerged as an alternative option to combat AD. To this date, dozens of MTDLs have been published. As part of the experimetnal section of this thesis, a series of small molecules based on quinazoline scaffold was rationally designed with the intention to influence the activity of acetylcholinesterase, butyrylcholinesterase, monoamine oxidase A and B (MAO-A/MAO-B), and the GluN1/GluN2B subunit of N-methyl-D-aspartate receptor (NMDAR). Subsequently twenty-four new quinazoline derivatives were synthesized, and biologically evaluated. The overall results highlighted compound II-6h ((5E)-8-chlor-N-cyklohexyl-3-methyl-1-...
The application of cycloisomerization and cycloaddition for the building of polycyclic scaffolds
Timoracký, Marek ; Matouš, Petr (advisor) ; Opálka, Lukáš (referee)
Charles University Faculty of Pharmacy in Hradec Králové Department of Organic and Bioorganic Chemistry Candidate: Marek Timoracký Supervisor: PharmDr. Petr Matouš, Ph.D. Title of thesis: The application of cycloisomerization and cycloaddition for the building of polycyclic scaffolds This diploma thesis deals with the use of gold-catalyzed cyclizations and Diels-Alder reactions in the preparation of complex cyclic structures. In the introductory part, the use of gold as a catalyst is discussed, especially in the cyclizations of double and triple bond containing compounds (enynes). This is followed by a review of the utilization of Diels-Alder cycloaddition in organic synthesis. The actual experimental work deals with the synthesis of tetrahydropyridine with vinyl substitution by Au(I)-cyclization and the use of this compound as a diene for the Diels-Alder reaction. For the synthesis of substituted tetrahydropyridine, 2 possible routes of preparation of starting compound for cyclization using Michael addition and Sonogashira cross-coupling were utilized and compared. The resulting tetrahydropyridine was subsequently subjected to various Diels-Alder reactions, to expand the chemical library with isomeric derivatives of isoquinoline, pyrrolo[3,4 h]isoquinoline and pyrano[2,3-c]pyridine. Keywords:...
Synthesis and evaluation of potential antimicrobial agents based on steroidal scaffold
Požárová, Pavla ; Krátký, Martin (advisor) ; Matouš, Petr (referee)
Antibiotic resistance represents a significant threat to humanity. To combat this trend, the development of new effective substances can be employed to potentially reverse its progression. Due to the broad range of biological activities exhibited by steroid structures, estrone was chosen as the starting material and was modified through various reactions. In total, fifteen new compounds were synthesized, which were tested for their antibacterial, antifungal, and antimycobacterial activities, and additionally for cholinesterases inhibition. The modification of estrone primarily involved two different approaches, resulting in the formation of hydrazones and esters. Twelve compounds were prepared through these steps. For the remaining three derivatives, changes in the starting materials or procedures were necessary. In the case of four compounds, it was necessary to synthesize one of the reactants. The yields ranged from 62% to 95% for hydrazones and from 8% to 54% for esters. The antibacterial activity was tested against four selected Gram-positive and Gram-negative strains. Antifungal activity was evaluated against four yeasts and filamentous fungi. Antimycobacterial activity was tested against five mycobacterial strains. All these methods utilized the microdilution broth method. The tested...
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.
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.
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 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 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 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.
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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2 MATOUŠ, Pavel
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