National Repository of Grey Literature 134 records found  1 - 10nextend  jump to record: Search took 0.01 seconds. 
Synthesis of photoactive derivatives of phthalocyanines and study of their biological activity
Rychvalská, Lucia ; Zimčík, Petr (advisor) ; Vícha, Robert (referee) ; Zitko, Jan (referee)
Charles University, Faculty of Pharmacy in Hradec Králové Department: Department of Pharmaceutical Chemistry and Pharmaceutical Analysis Author: Mgr. Lucia Rychvalská Supervisor: prof. PharmDr. Petr Zimčík, PhD. Doctoral Thesis: Synthesis of photoactive derivatives of phthalocyanines and study of their biological activity Phthalocyanines (Pc) are macrocyclic compounds with conjugated system of double bonds with absorption maximum around 650 - 750 nm. They are characterized by high singlet oxygen production which makes them suitable candidates for photosensitizers in photodynamic therapy. However, they form inactive aggregates in water environment because of their planar hydrophobic aromatic core. There are many strategies to solve this problem, and this thesis is focused on fighting aggregation of Pc by their supramolecular interactions with cucurbiturils (CB). Subphthalocyanines (SubPc) are similar macrocyclic compounds composed of only three (instead of four) isoindol units with boron as a central atom, which has also axial substituent. Because of their cone-shape and axial substituent they are less aggregated in water but usually not very soluble, which could also be solved by interaction with CB. First part of this thesis was focused on synthesis of Pc with aminoadamantyl substituents on...
Design, synthesis and evaluation of heterocyclic compounds with potential antimicrobial activity I
Brányik, Michal ; Zitko, Jan (advisor) ; Demuth, Jiří (referee)
Charles University, Faculty of Pharmacy in Hradec Králové Department of Pharmaceutical Chemistry and Pharmaceutical Analysis Title of the thesis: Design, synthesis and evaluation of heterocyclic compounds with potential antimicrobial activity I Author: Michal Brányik Supervisor: doc. PharmDr. Jan Zitko, Ph.D. Consultant: PharmDr. Martin Juhás, Ph.D. Antimicrobial resistance is an ever-growing problem that occurs worldwide. Many bacterial strains develop the ability to resist the otherwise efficient substances, thus posing a serious threat for the future. Mycobacterium tuberculosis (Mtb), the source of tuberculosis, is no exception. Given that it is the leading cause of death due to a single pathogen, many efforts have been put into finding new active compounds. The substances synthesized as a part of this thesis are based on previously prepared substances with potential antimicrobial activity. The basic structure consists of 2-aminooxazole or 2-aminothiazole and substituted pyridine or pyrazine carboxamides. The structures were confirmed by the 1 H and 13 C NMR spectra, IR spectra and mass spectrometry. All the substances were tested for in vitro activity against eight bacterial strains (four gram-positive and four gram-negative) as well as eight fungal strains (four yeast and four fungi). We also...
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...
Preparation of fluorescent phthalocyanines for labeling of oligonucleotide probes IV.
Mikula, Daniel ; Miletín, Miroslav (advisor) ; Zitko, Jan (referee)
Charles University, Faculty of Pharmacy in Hradec Králové Department Department of Pharmaceutical Chemistry and Pharmaceutical Analysis Candidate Daniel Mikula Supervisor doc. PharmDr. Miroslav Miletín, Ph.D. Consultant Mgr. Michaela Kolářová Title of thesis Preparation of fluorescent phthalocyanines for labeling of oligonucleotide probes IV. Phthalocyanines (Pcs) are macrocyclic compounds with a conjugated system of double bonds. Thanks to this, they have interesting photophysical and photochemical properties that enable their practical use in pharmacy and medicine in the field of diagnostics or treatment of cancer diseases. This work deals with the preparation of axially disubstituted silicon complexes of phthalocyanines (SiPcs), which would have suitable properties for subsequent use in the labeling of oligonucleotide probes. The theoretical part is primarily devoted to the methods of Pcs preparation, from the choice of precursors, through the formation of the macrocycle and insertion of the central atom, to the modifications of the resulting molecule, including the specifics related to SiPcs. The basic properties of Pcs and the degree of influence of different changes of the molecule on these properties are also described. The basic areas of use of Pcs are also mentioned. The experimental part...
Design, synthesis and evaluation of heterocyclic compounds with potential antimicrobial activity VI
Abdalrahman, Nechirwan Taimur ; Zitko, Jan (advisor) ; Nováková, Veronika (referee)
(In English) Charles University Faculty of Pharmacy in Hradec Králové Department of Pharmaceutical Chemistry and Pharmaceutical Analysis Author: Nechirwan Abdalrahman Supervisor: Assoc. Prof. PharmDr. Jan Zitko, Ph.D. Title: Design, synthesis, and evaluation of heterocyclic compounds with potential antimicrobial activity VI Despite the existence of a well-established treatment regimens, tuberculosis (TB) continues to be the most leading cause of death by a single microorganism, as reported by WHO. One of the reasons behind treatment failure in completely eradicating this infection is drug resistance. Novel 3-(phenylureido)pyrazine-2-carboxamide derivatives, refer to figure below, were synthesized by reacting 3-chloropyrazine-2-carboxamide with ammonia to produce 3- aminopyrazine-2-carboxamide as an intermediate building block, followed by reacting with various substituted phenyl isocyanates using a microwave reactor. The synthesized compounds were evaluated for in vitro activity against various mycobacterial strains, where most active ones among them showed moderate to low activities; 4-tertiary butyl (MIC 62.5 µg/mL), 4-NO2 (MIC 62.5 µg/mL), 4-Bromo (MIC 250 µg/mL), 4-Cl (MIC 250 µg/mL), 2-F (MIC 250 µg/mL), and non-substituted (MIC 500 µg/mL). As a complementary study in silico, the synthesized...
Design, synthesis and evaluation of heterocyclic compounds with potential antimicrobial activity IV
Fekri, Amir Hossein ; Zitko, Jan (advisor) ; Miletín, Miroslav (referee)
(English) Charles University, Faculty of Pharmacy in Hradec Králové Department of Pharmaceutical Chemistry and Pharmaceutical Analysis Thesis title: Design, synthesis and evaluation of heterocyclic compounds with potential antimicrobial activity IV Candidate: Amirhossein Fekri Supervisor: doc. PharmDr. Jan Zitko, Ph.D. Consultant: Mgr. Vinod S. K. Pallabothula Tuberculosis has remained one of the deadliest infectious diseases worldwide caused by a single infectious agent, the rapid growth of resistance to anti-tubercular drugs hinders the successful control and treatment of TB worldwide, which challenges the scientific community to develop new drugs to improve currently available treatment. This diploma thesis represents the design, synthesis, and biological evaluation of two series of compounds including cyclized (pyrazine- oxazinone) and carboxamide derivatives as potentially active antimycobacterial agents sharing a pyrazine core as common structural features that could potentially target mycobacterial aspartate decarboxylase (PanD) and prolyl-tRNA synthetase (mtProRS), respectively. Synthesis of final compounds was achieved through individual reaction steps involving acylation of methyl 3-aminopyrazine-2-carboxylate for preparation of a common intermediate which in turn was used for the...
Synthesis of substituted aminoadamantyl compounds
Janišová, Denisa ; Zimčík, Petr (advisor) ; Zitko, Jan (referee)
Charles University, Faculty of Pharmacy in Hradec Králové Deparment: Department of Pharmaceutical Chemistry and Pharmaceutical Analysis Candidate: Denisa Janišová Supervisor: prof. PharmDr. Petr Zimčík, Ph.D. Advisor: Mgr. Lucia Rychvalská Title of Thesis: Synthesis of substituted aminoadamantyl compounds This work deals with the topic of photodynamic therapy using phthalocyanines as photosensitizers. The theoretical part summarizes the basic knowledge and findings about photodynamic therapy, its principle, application and used photosensitizers. Phthalocyanines (Pcs), their structure and possible variations, their synthesis and aggregation are also described.The last part is dedicated to cucurbiturils,which form stronghost-guest complexes with small molecules,in our case with aminodamantanes.These complexes mayincrease the monomerization and solubility of phthalocyanines in water. In the experimental part of the work, attention was focused on the synthesis of 1-aminoadamantane substituted by thiol group on two-carbon linker. However, synthesis of this compound was not successful anddespite number ofalternativeapproaches we were not able to prepare it. The reactions ran better in case of extension ofthe linker to three carbons and 3-((adamant-1-yl)amino)propan-1-thiol was succesfully synthesized by...
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 of thiazolidine derivatives as potential drugs
Makovská, Kateřina ; Kučerová, Marta (advisor) ; Zitko, Jan (referee)
Charles University Faculty of Pharmacy in Hradec Králové Department of Pharmaceutical Chemistry and Pharmaceutical Analysis Title of diploma thesis: Synthesis of thiazolidine derivatives as potential drugs Student: Kateřina Makovská Supervisor: PharmDr. Marta Kučerová, Ph.D. The theoretical part was focused on the literature research on the biological activity of derivatives 2-thioxothiazolidine-4-one (rhodanine) and its oxygen isostere thiazoli- dine-2,4-dione. There was mainly the antibacterial, antimycobacterial, and antifungal activity of variously substituted rhodanine and thiazolidine-2,4-dione derivatives repor- ted. These derivatives seem to be suitable candidates for the development of new drugs Within the experimental part, an in silico study on molecular docking of a larger series of rhodanine and thiazolidine-2,4-dione derivatives prepared in this work and earlier was performed with MurD ligase of E. coli as a potential bacterial target. On the whole, seventeen syntheses were performed in the laboratory using the Kno- evenagel condensation of thiazolidine-2,4-dione or rhodanine with various aldehydes, nine reactions with the aim to obtain thiazolidine-2,4-dione derivatives and eight reacti- ons withe the goal to get rhodanine derivatives. Eleven reactions afforded successfully six...
Design, synthesis and evaluation of heterocyclic compounds with potential antimicrobial activity I
Brányik, Michal ; Zitko, Jan (advisor) ; Demuth, Jiří (referee)
Charles University, Faculty of Pharmacy in Hradec Králové Department of Pharmaceutical Chemistry and Pharmaceutical Analysis Title of the thesis: Design, synthesis and evaluation of heterocyclic compounds with potential antimicrobial activity I Author: Michal Brányik Supervisor: doc. PharmDr. Jan Zitko, Ph.D. Consultant: PharmDr. Martin Juhás, Ph.D. Antimicrobial resistance is an ever-growing problem that occurs worldwide. Many bacterial strains develop the ability to resist the otherwise efficient substances, thus posing a serious threat for the future. Mycobacterium tuberculosis (Mtb), the source of tuberculosis, is no exception. Given that it is the leading cause of death due to a single pathogen, many efforts have been put into finding new active compounds. The substances synthesized as a part of this thesis are based on previously prepared substances with potential antimicrobial activity. The basic structure consists of 2-aminooxazole or 2-aminothiazole and substituted pyridine or pyrazine carboxamides. The structures were confirmed by the 1 H and 13 C NMR spectra, IR spectra and mass spectrometry. All the substances were tested for in vitro activity against eight bacterial strains (four gram-positive and four gram-negative) as well as eight fungal strains (four yeast and four fungi). We also...

National Repository of Grey Literature : 134 records found   1 - 10nextend  jump to record:
See also: similar author names
1 Zítko, Jakub
Interested in being notified about new results for this query?
Subscribe to the RSS feed.