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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 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...
Synthesis of coumarin based fluorophore probes
Koutníková, Barbora ; Doležal, Martin (advisor) ; Nováková, Veronika (referee)
Charles University Department of Pharmaceutical Chemistry and Pharmaceutical Analysis Student: Barbora Koutníková Supervisor: prof. PharmDr. Martin Doležal, Ph.D. Consultant: prof. Janez Ilaš, M. Pharm., Ph.D. Title of diploma thesis: Synthesis of coumarin based fluorophore probes Cancer remains to be one of the leading causes of death worldwide. Despite the progress in anti-cancer treatment, therapy of cancer is still associated with many disadvantages including an absence of selectivity as a major issue. The aim in development of chemotherapeutic drugs is to prepare more selective and better tolerated anti-cancer agents. Topoisomerases play an important role in the therapy of bacterial infections as well as anti-cancer treatment. Both types (human topo I and II) can be targeted during anti-cancer therapy. Isoform IIα is overexpressed during proliferation of the cell and therefore it is characteristic for cancer cells. Inhibition of this isoform leads to excessive DNA damage or to malfunctions during cell proliferation and consequently to cell apoptosis. This is why inhibitors of topoisomerase IIα are studied as candidates for anti-cancer therapy. The aim of this work was to prepare three compounds that would be later tested for inhibitory activity on human topoisomerase IIα. Optimization of the...
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...
DNS firewall and its deployment and integration in cyber center
Doležal, Martin ; Kubánková, Anna (referee) ; Jeřábek, Jan (advisor)
This bachelor's thesis deals with the deployment, integration, and testing of a DNS firewall in a security operations center. It describes the connection of endpoints and remote local area networks to the DNS firewall located in the security operations center. Furthermore, the enforcement of the DNS firewall is described. The main goal of the thesis was to deploy and integrate a DNS firewall inside a security operations center. The first chapter describes the security operations center in general. The second chapter deals with the DNS system. The following chapter describes the security of the DNS system and security of DNS requests, the reader is informed of the term DNS firewall and RPZ and VPN technologies. The fourth chapter describes the DNS firewall deployment process and its integration in a real security operations center. The next chapter describes connection methods of endpoint and remote local area networks to the DNS firewall and its enforcement inside the security operations center. The last chapter deals with performance testing and deployed DNS firewall availability. The outcome of the thesis involves a deployed, integrated, fully-functional, and tested DNS firewall in a real-world security operations center. The Bind software package along with the RPZ technology was used to implement and deploy the DNS firewall. For testing and connection of endpoints, the VPN technology, and the RIPE Atlas network was used.
Study of alkali metals ions diffusion in hardened cement
Doležal, Martin ; Janča, Martin (referee) ; Šoukal, František (advisor)
This master thesis is aim to study alkali diffusion (sodium, potassium) in hardened cement paste body. It´s deal with impact of various sorroudings (hydroxide, nitrate and carbonate) in various concentrations and temperature effect. This work is also deal with changes in cement paste and medium. Teoretic part is talking about cement production and cement chemistry, alkali-silica reaction, plasticizer, diffusion an cement testing metods. This work is aimed to white (Aalborg CEM I 52,5 R – SR 5) and road (Mokrá CEM I 42,5 R – sc) cement. Experimental part describes constitution of tested cement pastes, conservation of them and sampling. Diffusion is study by ICP-AES which affected the loss of alkali from the solution and SEM which affected alkali migration (diffusion) in cement paste. In several cases, the formation of a saturated alkali edge was observed, followed by steady diffusion. In the case of potassium there was very slow diffusion through the body mass. The influence of medium and temperature was evaluated as the most significant. The effect of medium concentration wasn´t significant. Also changes in the porosity on the body were observed. The diffusion itself was affected by secondary products gorwing on the surface of body and in the medium. The work deals with them in the last part.
Pyrazine derivatives as potential drugs III
Hošťálková, Anna ; Doležal, Martin (advisor) ; Kopecký, Kamil (referee)
Deriváty pyrazinu jako potanciální léčiva III. Tuberkulóza je problém v celosvětovém měřítku. Rostoucí počet nakažených lidí, vznik lékově rezistentních kmenů Mycobacterium tuberculosis a ko-infekce HIV vedly k naléhavé potřebě nových antituberkulotik. Tato diplomová práce referuje o současných léčivech používaných při léčbě tuberkulózy a některých nových potenciálních antituberkuloticích. Také bylo v rámci diplomové práce syntetizováno deset nových látek, derivátů anilidů kyseliny pyrazin-2-karboxylové, které byly charakterizovány jejich fyzikálními vlastnostmi a poté byla zkoušena jejich antimykobakteriální a antifungální aktivita in vitro. Abstract Pyrazine derivatives as potential drugs III. Tuberculosis is a health problem worldwide. The increasing number of infected people, emergence of drug resistant strains Mycobacterium tuberculosis and HIV co-infection have resulted in the urgent need for new antituberculosis drugs. This degree work reviews drugs used in current treatment for tuberculosis and some of new potential anti-tuberculosis drug candidates. Within the task of this work were also synthesized ten new compounds, derivatives of anilides of pyrazin-2-carboxylic acid, which were characterized by physical properties and then was assayed their antimycobacterial and antifungal activity in...

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