National Repository of Grey Literature 75 records found  1 - 10nextend  jump to record: Search took 0.01 seconds. 
Acyclic nucleosides of 3-hydroxypyrazine-2-carboxamide bases
Chaloupecká, Ema ; Jindřich, Jindřich (advisor) ; Smrček, Stanislav (referee)
This thesis deals with the preparation of acyclic nucleosides and nucleoside phosphonates of compounds T-705 (6-fluoro-3-hydroxypyrazine-2-carboxamide) and T-1105 (3-hydroxypyrazine-2-carboxamide). Acyclic nucleoside phosphonates are substances that can terminate viral RNA or DNA replication, and some of them are used in the treatment of viral diseases. T-705 and T-1105 have shown activity against the influenza virus, and T-705 has already been approved for its treatment in Japan. Since both compounds mimic natural nucleobases in the body, their acyclic nucleosides and nucleoside phosphonates also have the potential to be biologically active. Methods for the synthesis of 3-fluoro-2-(phosphonomethoxy)propyl and 3-hydroxy-2-(phosphonomethoxy)propyl derivatives of T-705 and T-1105, their prodrugs containing lipophilic groups for the improvement of the pharmacokinetic properties and also their phosphonate diphosphates, suitable for the biological activity measurements, have been proposed. Some of these derivatives were subsequently prepared. Key words: acyclic nucleosides, acyclic nucleoside phosphonates, T-705, T-1105, favipiravir, antiviral activity, influenza
Binding constants of fluorophores with cyclodextrins
Křeček, Tomáš ; Jindřich, Jindřich (advisor) ; Veselý, Jan (referee)
This thesis deals with the preparation of fluorophores - substituted naphtalendiimides, where the starting compound of the synthesis is 1,4,5,8-naphtalentetracarboxylic acid. Due to their structure, cyclodextrins have the ability include substances into their non-polar cavity, which was used to form a complex of β-cyclodextrin with the prepared 2,6- diaminopropyl-1,4,5,8-naftalenpropyldidiimide. Binding constant of complex was measured at optimized conditions in a methanol/water mixture. Keywords: binding constants, cyclodextrins, fluorophores
Synthesis of cyclodextrin derivatives for organocatalysis
Chena Tichá, Iveta ; Jindřich, Jindřich (advisor) ; Lhoták, Pavel (referee) ; Šindelář, Vladimír (referee)
Synthesis of cyclodextrin derivatives for organocatalysis This doctoral thesis examines the preparation of new cyclodextrin (CD) derivatives suitable for organocatalysis. The aim of this work is to prepare monosubstituted and disubstituted CD derivatives as organocatalysts for different types of enantioselective reactions potentially performed in water. In addition, disubstituted CD derivatives require considering the potential mixture of regioisomers and pseudoenantiomers. Thus, this thesis is divided into several sections - preparation of CD precursors and derivatives for organocatalysis, preparation of pure regioisomers and pseudoenantiomers of disubstituted CDs and final application of CD derivatives in enantioselective reactions. Furthermore, this thesis also focuses on the molecular modeling of the prepared CD derivatives and on their catalytic activity in silico. The first section covers the preparation of new disubstituted CD precursors as pure regioisomers for organocatalysts, specifically to develop a new method for the preparation of heterodisubstituted AC regioisomers on the primary rim of α-CD. This section also includes the determination of the regioisomer ratios of common α-CD intermediates disubstituted on the primary rim to evaluate their potential as precursors in organocatalysis....
2-(Phosphonomethoxy)ethyl derivatives of 6-fluoro-3-hydroxypyrazine-2-carboxamide
Lamačová, Lucie Josefa ; Jindřich, Jindřich (advisor) ; Baszczyňski, Ondřej (referee)
This bachelor thesis deals with the preparation of derivatives of acyclic nucleoside phosphonates with nitrogenous base favipiravir. There are many examples of acyclic nucleoside phosphonates that are used as antiviral drugs due to their structure. Favipiravir shows antiviral activity against the influenza virus. The target compounds thus might have the potential to be biologically active, which will be tested in virological laboratories at KU Leuven in Belgium. First, the methods for preparation of 2-(phosphonomethoxy)ethyl derivative of favipiravir was designed, then for its diphosphate and a prodrug with pivaloyloxymethyl groups to increase the bioavailability of the compound. Thus, 2-(phosphonomethoxy)ethyl derivatives of favipiravir and its de-fluoro analogue were prepared. Key words: acyclic nucleoside phosphonates, T-705, favipiravir, T-1105, influenza, antiviral activity
Synthesis of five-membered ring analogues of Amaryllidaceae alkaloids
Kvapilová, Pavlína ; Matoušová, Eliška (advisor) ; Jindřich, Jindřich (referee)
This bachelor Thesis deals with the synthesis of polycyclic compounds containing all-carbon quaternary centres. Quaternary centres with a similar substitution as our target compounds can be found in some natural products. In particular, nitrogen-containing compounds, structurally related to Amaryllidaceae alkaloids, have been prepared in this work. For the construction of the all-carbon quaternary centre we used tandem cyclization/Suzuki cross-coupling and halocarbocyclisation reaction sequence. The first part of the Thesis is dedicated to compounds that have a nitrogen atom protected by a p-methoxybenzenesulfonyl group. In the second part we deal with the preparation of N-methyl derivatives of these compounds. The third part is dedicated to the synthesis of a protected amine from 2-oxazolidinone, which we have unsuccessfully used for the preparation of polycyclic compounds with a hydroxyethyl group on the nitrogen atom. Key words: Synthesis, Amaryllidaceae alkaloids, polycyclic compounds, biological activity
Synthesis of fluorophores with permanent positive charges for construction of chemosensors on solid phase
Smolka, Ondřej ; Jindřich, Jindřich (advisor) ; Matoušová, Eliška (referee)
This bachelor work is focused on the synthesis of fluorophores with two positive charges based on 1,2,3-triazole motive. The work deals with optimalization of their synthetic processes and characterization of the compounds. Optical properties of the double charged fluorophores and their complexation ability with -cyclodextrin were studied. Key words: 1,2,3-triazoles, charged fluorophores, positive charges, cyclodextrines, complexation
Cyclodextrin derivatives containing covalently bound volatile substances and studies of their release
Palágyi, Attila ; Jindřich, Jindřich (advisor) ; Smrček, Stanislav (referee)
The main aim of the work was to prepare a series of β-cyclodextrin derivatives containing covalently bound volatile compounds via an imine bond. The used volatile compounds were cinnamaldehyde, cyclamen aldehyde, lilal, benzaldehyde, anisaldehyde, vanillin, hexanal, heptanal, citral and 5-methylfurfural. Subsequently, the rate of the release of the active compound, as a function of the environment, was studied by 1 H NMR spectroscopy and static headspace-gas chromatography. Key words: cyclodextrin, aldehyde, imine, kinetics, controlled release
Effect of perfluoroalkyl substituents onthe formation and costitutional dynamics of Schiff bases
Štrympl, Ondřej ; Vohlídal, Jiří (advisor) ; Jindřich, Jindřich (referee)
New synthetic routes were designed and applied for novel bisperfluoroalkylated benzene derivatives: 2,5-bis(perfluorooctyl)benzene-1,4-dicarbaldehyde, its dimethylacetal and 2,5- bis(trifluoromethyl)benzene-1,4-diamine. Methods for purification of those derivatives were developed and used to obtain pure crystalline compounds. Crystals of the mentioned diamine and diacetal were obtained in quality suitable for RTG analysis while crystals of dialdehyde were of sufficient quality. New synthesis and purification protocol was designed for 2,5-bis(trifluoromethyl)benzene- 1,4-dialdehyde yielding sufficiently pure product, although isolated amounts are rather small ( yields about 20%) . 2,5-diiodobenzene-1,4-diamine was synthetised. It should be possible to prepare 2,5- bis(perfluorooktyl)benzene-1,4-diamine from this compound either by direct or indirect approach. Nevertheless, the syntheses were yet unsuccessful. A series of eight Schiff bases derived from 3,5-bistrifluoromethylated benzeneamine, benzylamine and benzaldehyde, and three reference bases based on thiophene-2-carbadehyde, benzaldehyde and phenylacetaldehyde was prepared. Kinetics of those species' formation in CDCl3 (all reactions run without catalyst) and THF (necessity of catalysis and susceptibility of equilibria to water) were studied. The...
Selectively substituted cyclodextrins for analytical and pharmaceutical applications
Benkovics, Gábor ; Jindřich, Jindřich (advisor) ; Lhoták, Pavel (referee) ; Šindelář, Vladimír (referee)
3 Selectively substituted cyclodextrins for analytical and pharmaceutical applications Abstract This thesis is focused on the selective modification of cyclodextrins, and its primary aim is the preparation and characterization of mono- and persubstituted derivatives of cyclodextrins in a regioselective and straightforward manner. The work is divided into two main parts describing synthetic strategies and applications of modified cyclodextrins with one or several substituents, respectively. The first section deals with the introduction of a single chromophoric moiety on the cyclodextrin scaffold such as cinnamyl, rhodaminyl, fluoresceinyl and eosinyl groups. The complete set of monocinnamyl-α-cyclodextrin regioisomers has been prepared by direct alkylation, and the self-assembling properties of the corresponding regioisomers were thoroughly investigated by dynamic light scattering and NMR experiments. These investigations revealed that the different isomers (mono-6-O-, mono-2-O- and mono-3-O- cinnamyl-α-cyclodextrin) form distinct supramolecular species through intermolecular association. A fast method for the unambiguous identification of the pure regioisomers has also been developed based on a series of 2D NMR measurements. Xanthene-modified β-cyclodextrins, other representatives of monosubstituted...

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3 Jindřich, Jan
1 Jindřich, Jaromír
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